Antibodies
LY404039
- 貨號 Cat. No.
- S6001
- 規格 Size
- 5mg~25mg
- 品牌 Brand
- Selleckchem
Description
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h1 itemprop=name style=margin: 0px 20px 0px 0px; padding: 0px; font-size: 24px; float: left;LY404039/h1
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/spana class=pro_a href=http://www.selleckchem.com/products/LY2140023(LY404039).html#customerReviews date-widget=scrollMove style=margin: 0px 15px 0px 0px; padding: 0px; text-decoration: none; color: rgb(52, 84, 140); cursor: pointer; float: left;span class=margin_l style=margin: 0px 0px 0px 10px; padding: 0px;2 Reviews/span/aa class=pro_a href=http://www.selleckchem.com/products/LY2140023(LY404039).html#productCitations date-widget=scrollMove style=margin: 0px 15px 0px 0px; padding: 0px; text-decoration: none; color: rgb(52, 84, 140); cursor: pointer; float: left;3 Product Citations/a/div
p class=new_title style=margin: 5px 0px 10px; padding: 0px; clear: both; font-size: 11px; line-height: 14.399999618530273px;LY404039 is a potent agonist of recombinant humannbsp;b style=margin: 0px; padding: 0px;mGlu2/mGlu3/bnbsp;receptors withnbsp;b style=margin: 0px; padding: 0px;Kspan style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: 0.25em;i/span/bnbsp;of 149 nM/92 nM, shows gt;100-fold selectivity over ionotropic glutamate receptors, glutamate transporters, and other receptors. Phase 3./p
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td width=139 style=margin: 0px; padding: 3px 8px;label style=margin: 0px; padding: 0px;5mg/label/td
td width=80 style=margin: 0px; padding: 3px 8px;USD 88/td
td width=62 style=margin: 0px; padding: 3px 8px;In stock/td
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td width=139 style=margin: 0px; padding: 3px 8px;label style=margin: 0px; padding: 0px;25mg/label/td
td width=80 style=margin: 0px; padding: 3px 8px;USD 340/td
td width=62 style=margin: 0px; padding: 3px 8px;In stock/td
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td width=80 style=margin: 0px; padding: 3px 8px;USD 592/td
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h3 id=biologicalActivity style=margin: 25px 0px 0px; padding: 0px; height: 25px; font-size: 14px; font-family: Arial, Tahoma, Helvetica; line-height: 19.200000762939453px;Biological Activity/h3
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th width=16% style=margin: 0px; padding: 5px 0px 5px 15px; font-weight: normal; border-style: solid; border-color: rgb(229, 229, 229);Description/th
td colspan=6 style=margin: 0px; padding: 5px 15px; text-align: justify; border-style: solid; border-color: rgb(229, 229, 229);LY404039 is a potent agonist of recombinant humannbsp;b style=margin: 0px; padding: 0px;mGlu2/mGlu3/bnbsp;receptors withnbsp;b style=margin: 0px; padding: 0px;Kspan style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: 0.25em;i/span/bnbsp;of 149 nM/92 nM, shows gt;100-fold selectivity over ionotropic glutamate receptors, glutamate transporters, and other receptors. Phase 3./td
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th style=margin: 0px; padding: 5px 0px 5px 15px; font-weight: normal; border-style: solid; border-color: rgb(229, 229, 229);Targets/th
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);Recombinant human mGlu2/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);Recombinant human mGlu3/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);Rat neurons expressing native mGlu2/3/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);nbsp;/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);nbsp;/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);nbsp;/td
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th style=margin: 0px; padding: 5px 0px 5px 15px; font-weight: normal; border-style: solid; border-color: rgb(229, 229, 229);IC50/th
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);149 nM (Kspan style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: 0.25em;i/span)/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);92 nM (Kspan style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: 0.25em;i/span)/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);88 nM (Kspan style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: 0.25em;i/span)nbsp;span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;a href=http://www.selleckchem.com/products/LY2140023(LY404039).html#s_ref class=sref style=margin: 0px; padding: 0px; text-decoration: none; color: rgb(52, 84, 140); cursor: pointer;[1]/a/span/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);nbsp;/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);nbsp;/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);nbsp;/td
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th style=margin: 0px; padding: 5px 0px 5px 15px; font-weight: normal; border-style: solid; border-color: rgb(229, 229, 229);i style=margin: 0px; padding: 0px;In vitro/i/th
td colspan=6 style=margin: 0px; padding: 5px 15px; text-align: justify; border-style: solid; border-color: rgb(229, 229, 229);LY404039 exhibits low binding affinity to group III mGlu receptors including mGlu6, mGlu7 and mGlu8 with a Kspan style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: 0.25em;i/spanvalue more than 5 mu;M. LY404039 shows little affinity for ionotropic glutamate receptors, glutamate transporter subtypes, monoamine and other receptors. LY404039 potently inhibits forskolin-stimulated cAMP formation in cells expressing human mGlu2 and mGlu3 receptors. LY404039 suppresses electrically evoked excitatory activity in the striatum, and serotonin-induced L-glutamate release in the prefrontal cortex. LY404039 could modulate glutamatergic activity in limbic and forebrain areas relevant to psychiatric disorders and may be devoid of negative side effects associated with current antipsychotics and anxiolytics.nbsp;span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;a href=http://www.selleckchem.com/products/LY2140023(LY404039).html#s_ref class=sref style=margin: 0px; padding: 0px; text-decoration: none; color: rgb(52, 84, 140); cursor: pointer;[1]/a/span/td
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th style=margin: 0px; padding: 5px 0px 5px 15px; font-weight: normal; border-style: solid; border-color: rgb(229, 229, 229);i style=margin: 0px; padding: 0px;In vivo/i/th
td colspan=6 style=margin: 0px; padding: 5px 15px; text-align: justify; border-style: solid; border-color: rgb(229, 229, 229);LY404039 demonstrates higher plasma exposure and better oral bioavailability. LY404039 may be valuable in the treatment of neuropsychiatric disorders, including anxiety and psychosis.nbsp;span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;a href=http://www.selleckchem.com/products/LY2140023(LY404039).html#s_ref class=sref style=margin: 0px; padding: 0px; text-decoration: none; color: rgb(52, 84, 140); cursor: pointer;[1]/a/spannbsp;In wild-type animals, LY404039 significantly reverses d-amphetamine(AMP)-induced increase in ambulations, distance traveled, and reduced time spent at rest. LY404039 reverses phencyclidine (PCP)-evoked behaviors at 10 mg/kg. The antipsychotic-like effects of LY404039 on PCP and AMP-evoked behavioral activation are absent in mGlu2 and mGlu2/3 but not in mGlu3 receptor-deficient mice. In contrast, clozapine and risperidone inhibit PCP-evoked behaviors in both wild-type and mGlu2/3 receptor-deficient mice.nbsp;span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;a href=http://www.selleckchem.com/products/LY2140023(LY404039).html#s_ref class=sref style=margin: 0px; padding: 0px; text-decoration: none; color: rgb(52, 84, 140); cursor: pointer;[2]/a/spannbsp;LY404039 reduces responding on the EtOH in the pavlovian spontaneous recovery (PSR) test and reduces the expression of an alcohol deprivation effect (ADE) during relapse, but does not affect EtOH responding under maintenance conditions. LY404039 inhibits the expression of alcohol seeking and relapse behavior without altering alcohol self-administration behavior.nbsp;span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;a href=http://www.selleckchem.com/products/LY2140023(LY404039).html#s_ref class=sref style=margin: 0px; padding: 0px; text-decoration: none; color: rgb(52, 84, 140); cursor: pointer;[3]/a/spanMoreover, LY404039 attenuates amphetamine- and phencyclidine-induced hyperlocomotion. LY404039 could inhibit conditioned avoidance responding and also reduces fear-potentiated startle in rats and marble burying in mice. Importantly, LY404039 does not produce sedative effects or motor impairment in the conditioned avoidance task. LY404039 also increases dopamine and serotonin release/turnover in the prefrontal cortex.nbsp;span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;a href=http://www.selleckchem.com/products/LY2140023(LY404039).html#s_ref class=sref style=margin: 0px; padding: 0px; text-decoration: none; color: rgb(52, 84, 140); cursor: pointer;[4]/a/span/td
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th style=margin: 0px; padding: 5px 0px 5px 15px; font-weight: normal; border-style: solid; border-color: rgb(229, 229, 229);Features/th
td colspan=6 style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);Under investigation as an exciting new medicine that may herald the arrival of third-generation antipsychotic drugs./td
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h3 id=protocol style=margin: 25px 0px 0px; padding: 0px; height: 25px; font-size: 14px; font-family: Arial, Tahoma, Helvetica; line-height: 19.200000762939453px;Protocolspan style=margin: 0px; padding: 0px; font-weight: normal;(Only for Reference)/span/h3
h4 style=margin: 0px; padding: 0px; font-family: Arial, Tahoma, Helvetica; font-size: 12px; line-height: 19.200000762939453px;Kinase Assay:nbsp;span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;a href=http://www.selleckchem.com/products/LY2140023(LY404039).html#s_ref class=sref style=margin: 0px; padding: 0px; text-decoration: none; color: rgb(52, 84, 140); cursor: pointer;[1]/a/span/h4
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th width=16% style=margin: 0px; padding: 5px 0px 5px 15px; font-weight: normal; border-style: solid; border-color: rgb(229, 229, 229);Receptor Binding Assays/th
td style=margin: 0px; padding: 5px 15px; text-align: justify; border-style: solid; border-color: rgb(229, 229, 229);LY404039 is dissolved in DMSO to make a 10 mM stock solution. Cell lines expressing human mGlu2, mGlu3, mGlu1a, mGlu5a, mGlu4a, mGlu6, mGlu7a, and mGlu8 receptors are derived and cultured in DMEM with 5% dialyzed fetal bovine serum, 1 mM glutamine, 1 mM sodium pyruvate, 50 mg/mL Geneticin, and 0.2 mg/mL hygromycin B. Confluent cultures are passaged weekly. These cells are referred to as rat glutamate transporter (RGT) cells. RGT cells are actually AV12-664 cells, which have been stably transfected with a glutamate transporter (GLAST) to prevent the accumulation of L-glutamate in the cell media. Membranes from mGlu receptor-expressing RGT cells are prepared by harvesting adherent cells from confluent T-150 flasks with a cell scraper. Cells and media are then placed in 50-mL conical tubes and centrifuged at 10span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;3/spannbsp;g for 5 min at 4 deg;C. The supernatant is removed, and the pellet is frozen at -10 deg;C until use. Frozen pellets are routinely thawed at room temperature for about 10 min when required. Washed cell membranes are prepared by adding 20 mL of 10 mM potassium phosphate buffer, pH 7.6 and 100 mM potassium bromide, at 5 deg;C and homogenizing with a tissuemizer for 15 s at 90% output. The homogenate is centrifuged at 4.8 times; 10span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;3/spannbsp;g at 5 deg;C for 10 min. This last step is repeated twice, the final pellet is resuspended in 10 mL of the same buffer and reserved on ice until initiating the binding assay. [span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;3/spanH]LY341495 Binding: Group II mGlu Receptors: [span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;3/spanH]LY341495 binding is assayed in a reaction mixture containing 10 mM potassium phosphate, pH 7.6, 100 mM potassium bromide, and 1nM [span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;3/spanH]LY341495 (final volume, 500 mL). The incubation is initiated by the addition of the membrane suspension (15 mg of membrane protein) and kept on ice for 30 min. Incubation is terminated by rapid filtration with a cell harvester through glass fiber Whatman GF/B filters prewet with the same potassium phosphate buffer assay buffer at 4 deg;C. The filters are washed 5 times with 1 mL of buffer. Filter sections are transferred to minivials, and 5 mL liquid scintillation cocktail is added to each vial. Vials are allowed to set for several hours before counting on a liquid scintillation counter. Protein concentrations are quantified by microassay. Nonspecific binding is determined in the presence of 1 mM L-glutamate. [span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;3/spanH]LY341495 Binding: Group III mGlu Receptors: Membranes from cells expressing recombinant human group III mGlu receptors are prepared the same as described for group II mGlu receptor membranes. To start the reaction, washed tissue (0.05ndash;0.20 mg of protein) is added to 10 nM [span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;3/spanH]LY341495 and LY404039 in assay buffer. The final assay volume is 0.5 mL. Nonspecific binding is defined with 1 mM L-glutamate or 1 mM L-serine-O-phosphate (for mGlu7a). Assay plates are incubated for 45 min on ice, and the reaction is terminated by rapid filtration (GF/B filters) and washed twice with 1 mL of ice-cold assay buffer. Filters are placed in minivials, scintillation cocktail is added and counting is done in a liquid scintillation counter. Protein concentration is determined using the microassay. [span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;3/spanH]LY341495 Binding to Rat Brain Membranes: Brain tissue is obtained by decapitating adult male Sprague-Dawley rats (150ndash;250g). The forebrain (cortex, striatum, and hippocampus) is used; the brain tissue is homogenized in 30 mM Tris-HCl buffer, pH 7.6 and 2.5 mM CaClspan style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: 0.25em;2/span, at 5 deg;C and washed 3 times by centrifugation. The material is incubated at 37 deg;C for 30 min followed by 3 more washes, finally resuspended in 10 volumes of buffer and frozen at -20 deg;C. Frozen pellets of rat brain homogenate are thawed on the day of assay and washed 3 times with ice-cold assay buffer (10 mM potassium phosphate containing 100 mM potassium bromide, pH 7.6). The tissue (0.02ndash;0.06 mg of protein) is added to deep-well polypropylene microtiter plates, which contain 1 nM [span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;3/spanH]LY341495 and LY404039 in assay buffer. The final assay volume is 0.5 mL. Nonspecific binding is defined with 1 mM L-glutamate. Assay plates are incubated for 30 minutes on ice, and bound and free radioligands are separated by rapid filtration with 5 times; 1 mL of ice-cold assay buffer using Whatman GF/B filters. Protein concentration is determined using the microassay./td
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h4 style=margin: 0px; padding: 0px; font-family: Arial, Tahoma, Helvetica; font-size: 12px; line-height: 19.200000762939453px;Animal Study:nbsp;span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;a href=http://www.selleckchem.com/products/LY2140023(LY404039).html#s_ref class=sref style=margin: 0px; padding: 0px; text-decoration: none; color: rgb(52, 84, 140); cursor: pointer;[2]/a/span/h4
table width=100% border=0 cellspacing=0 cellpadding=0 class=product_show_table style=margin: 0px; padding: 0px; border-collapse: collapse; border-spacing: 0px; border-style: solid; border-color: rgb(229, 229, 229); color: rgb(0, 0, 0); font-family: Arial, Tahoma, Helvetica; font-size: 12px; line-height: 19.200000762939453px;
tbody style=margin: 0px; padding: 0px;
tr style=margin: 0px; padding: 0px;
th width=16% style=margin: 0px; padding: 5px 0px 5px 15px; font-weight: normal; border-style: solid; border-color: rgb(229, 229, 229);Animal Models/th
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);Separate mGlu2 and mGlu3 receptor knockout mice are established./td
/tr
tr style=margin: 0px; padding: 0px;
th width=16% style=margin: 0px; padding: 5px 0px 5px 15px; font-weight: normal; border-style: solid; border-color: rgb(229, 229, 229);Dosages/th
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);10 mg/kg/td
/tr
tr style=margin: 0px; padding: 0px;
th width=16% style=margin: 0px; padding: 5px 0px 5px 15px; font-weight: normal; border-style: solid; border-color: rgb(229, 229, 229);Administration/th
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);Administered via i.p./td
/tr
tr style=margin: 0px; padding: 0px;
th width=16% style=margin: 0px; padding: 5px 0px 5px 15px; font-weight: normal; border-style: solid; border-color: rgb(229, 229, 229);Solubility/th
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);30% propylene glycol, 5% Tween 80, 65% D5W, 30 mg/mL/td
/tr
/tbody
/table
pa id=s_ref style=margin: 0px; padding: 0px; color: rgb(52, 84, 140); cursor: pointer; font-family: Arial, Tahoma, Helvetica; line-height: 19.200000762939453px; clear: both; float: left; height: 0px; font-size: 0px;1/a/p
h4 class=reference margin_t style=margin: 10px 0px 0px; padding: 0px; font-family: Arial, Tahoma, Helvetica; font-size: 12px; line-height: 19.200000762939453px;References/h4
h3 id=clinical style=margin: 25px 0px 0px; padding: 0px; height: 25px; font-size: 14px; font-family: Arial, Tahoma, Helvetica; line-height: 19.200000762939453px;Clinical Trial Informationspan class=inpo style=margin: 0px 0px 0px 10px; padding: 0px; font-size: 12px; font-weight: normal;( data from http://clinicaltrials.gov)/span/h3
table width=100% border=0 cellspacing=0 cellpadding=0 class=inpo_table style=margin: 0px; padding: 0px; border-collapse: collapse; border-spacing: 0px; border-style: solid; border-color: rgb(229, 229, 229); color: rgb(0, 0, 0); font-family: Arial, Tahoma, Helvetica; font-size: 12px; line-height: 19.200000762939453px;
tbody style=margin: 0px; padding: 0px;
tr style=margin: 0px; padding: 0px;
th width=15% style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229); background-color: rgb(249, 249, 249);NCT Number/th
th width=12% style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229); background-color: rgb(249, 249, 249);Recruitment/th
th width=35% style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229); background-color: rgb(249, 249, 249);Conditions/th
th width=19% style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229); background-color: rgb(249, 249, 249);Sponsorbr style=margin: 0px; padding: 0px; /
/Collaborators/th
th width=10% style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229); background-color: rgb(249, 249, 249);Start Date/th
th width=9% style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229); background-color: rgb(249, 249, 249);Phases/th
/tr
tr style=margin: 0px; padding: 0px;
td style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229);NCT01475136/td
td style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229);Completed/td
td style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229);Hepatic Insufficiency/td
td style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229);Eli Lilly and Company/td
td style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229);2011-11/td
td style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229);Phase 1/td
/tr
tr style=margin: 0px; padding: 0px;
td style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229);NCT01591330/td
td style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229);Completed/td
td style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229);Healthy Volunteers/td
td style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229);Eli Lilly and Company/td
td style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229);2012-04/td
td style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229);Phase 1/td
/tr
tr style=margin: 0px; padding: 0px;
td style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229);NCT01609218/td
td style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229);Completed/td
td style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229);Healthy Volunteer Study/td
td style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229);Eli Lilly and Company/td
td style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229);2012-05/td
td style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229);Phase 1/td
/tr
tr style=margin: 0px; padding: 0px;
td style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229);NCT01637142/td
td style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229);Completed/td
td style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229);Healthy Participants/td
td style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229);Eli Lilly and Company/td
td style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229);2012-07/td
td style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229);Phase 1/td
/tr
tr style=margin: 0px; padding: 0px;
td style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229);NCT01659177/td
td style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229);Withdrawn/td
td style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229);Healthy Participants/td
td style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229);Eli Lilly and Company/td
td style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229);2012-08/td
td style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229);Phase 1/td
/tr
/tbody
/table
h3 id=chemicalInformation style=margin: 25px 0px 0px; padding: 0px; height: 25px; font-size: 14px; font-family: Arial, Tahoma, Helvetica; line-height: 19.200000762939453px;Chemical Information/h3
pa href=http://file.selleckchem.com/downloads/product-sdf/ly2140023-ly404039-s6001.SDF style=margin: -25px 0px 0px 180px; padding: 0px; text-decoration: none; color: rgb(52, 84, 140); cursor: pointer; font-family: Arial, Tahoma, Helvetica; font-size: 12px; line-height: 19.200000762939453px; float: left;Download LY404039 SDF/a/p
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tbody style=margin: 0px; padding: 0px;
tr style=margin: 0px; padding: 0px;
th width=45% style=margin: 0px; padding: 5px 0px 5px 15px; font-weight: normal; border-style: solid; border-color: rgb(229, 229, 229);Molecular Weight (MW)/th
td width=55% style=margin: 0px; padding: 5px 0px 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);235.22/td
/tr
tr style=margin: 0px; padding: 0px;
th width=45% style=margin: 0px; padding: 5px 0px 5px 15px; font-weight: normal; border-style: solid; border-color: rgb(229, 229, 229);Formula/th
td style=margin: 0px; padding: 5px 0px 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);
p style=margin: 0px; padding: 0px;Cspan style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: 0.25em;7/spanHspan style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: 0.25em;9/spanNOspan style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: 0.25em;6/spanS/p
/td
/tr
tr style=margin: 0px; padding: 0px;
th width=45% style=margin: 0px; padding: 5px 0px 5px 15px; font-weight: normal; border-style: solid; border-color: rgb(229, 229, 229);CAS No./th
td style=margin: 0px; padding: 5px 0px 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);635318-11-5/td
/tr
/tbody
/table
table width=100% border=0 cellspacing=0 cellpadding=0 class=show_tab fr style=margin: 0px 0px 10px; padding: 0px; border-collapse: collapse; border-spacing: 0px; width: 375px; float: right;
tbody style=margin: 0px; padding: 0px;
tr style=margin: 0px; padding: 0px;
th rowspan=2 valign=top class=padding5 style=margin: 0px; padding: 5px 0px 5px 10px; font-weight: normal; border-style: solid; border-color: rgb(229, 229, 229);Storage/th
td class=padding5 style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229);3 yearsnbsp;span class=margin_l style=margin: 0px 0px 0px 10px; padding: 0px;-20℃/spanspan class=margin_l style=margin: 0px 0px 0px 10px; padding: 0px;Powder/span/td
/tr
tr style=margin: 0px; padding: 0px;
td class=padding5 style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229);6 monthsspan class=margin_l style=margin: 0px 0px 0px 10px; padding: 0px;-80℃/spanspan class=margin_l style=margin: 0px 0px 0px 10px; padding: 0px;in DMSO/span/td
/tr
tr style=margin: 0px; padding: 0px;
th width=161 valign=top class=padding5 style=margin: 0px; padding: 5px 0px 5px 10px; font-weight: normal; border-style: solid; border-color: rgb(229, 229, 229);Syonnyms/th
td width=214 class=padding5 style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229);N/A/td
/tr
/tbody
/table
div class=clear-both style=margin: 0px; padding: 0px; clear: both; height: 0px; overflow: hidden;nbsp;/div
table width=100% border=0 cellspacing=0 cellpadding=0 class=product_show_table mb15 style=margin: 0px 0px 15px; padding: 0px; border-collapse: collapse; border-spacing: 0px; border-style: solid; border-color: rgb(229, 229, 229);
tbody style=margin: 0px; padding: 0px;
tr style=margin: 0px; padding: 0px;
th width=12% rowspan=4 style=margin: 0px; padding: 5px 0px 5px 15px; font-weight: normal; border-style: solid; border-color: rgb(229, 229, 229);strong style=margin: 0px; padding: 0px;Solubility (25deg;C)nbsp;/strongspan class=red style=margin: 0px; padding: 0px; color: rgb(255, 0, 0);*/span/th
td width=10% rowspan=3 class=italic style=margin: 0px; padding: 5px 15px; font-style: italic; border-style: solid; border-color: rgb(229, 229, 229);In vitro/td
td width=50% style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);DMSO/td
td width=28% style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);1 mg/mL (4 mM)/td
/tr
tr style=margin: 0px; padding: 0px;
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);Water/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);lt;1 mg/mL (lt;1 mM)/td
/tr
tr style=margin: 0px; padding: 0px;
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);Ethanol/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);lt;1 mg/mL (lt;1 mM)/td
/tr
tr style=margin: 0px; padding: 0px;
td class=italic style=margin: 0px; padding: 5px 15px; font-style: italic; border-style: solid; border-color: rgb(229, 229, 229);In vivo/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);30% propylene glycol, 5% Tween 80, 65% D5W,/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);30 mg/mL/td
/tr
tr style=margin: 0px; padding: 0px;
td colspan=4 style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);span class=red style=margin: 0px; padding: 0px; color: rgb(255, 0, 0);*/spannbsp;lt;1 mg/ml means slightly soluble or insoluble.br style=margin: 0px; padding: 0px; /
span class=red style=margin: 0px; padding: 0px; color: rgb(255, 0, 0);*/spannbsp;Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations./td
/tr
/tbody
/table
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tr style=margin: 0px; padding: 0px;
th width=153px style=margin: 0px; padding: 5px 0px 5px 15px; font-weight: normal; border-style: solid; border-color: rgb(229, 229, 229);Chemical Name/th
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);(1R,4S,5S,6S)-4-[[(2S)-2-Amino-4-(methylthio)-1-oxobutyl]amino]-2-thiabicyclo[3.1.0]hexane-4,6-dicarboxylic acid 2,2-dioxide/td
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Click to enlarge/a/td
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td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);Source/td
td class=italic style=margin: 0px; padding: 5px 15px; font-style: italic; border-style: solid; border-color: rgb(229, 229, 229);PLoS One, 2011, 6(7), e22235.span style=margin: 0px; padding: 0px; font-style: normal;nbsp;LY404039 purchased from Selleck/span/td
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tr style=margin: 0px; padding: 0px;
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);Method/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);Western Blot/td
/tr
tr style=margin: 0px; padding: 0px;
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);Cell Lines/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);astrocytes/td
/tr
tr style=margin: 0px; padding: 0px;
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);Concentrations/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);100 uM/td
/tr
tr style=margin: 0px; padding: 0px;
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);Incubation Time/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);30 min/td
/tr
tr style=margin: 0px; padding: 0px;
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);Results/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);LY404039 also induced Akt phosphorylation per se(Fig. A and B). As a negative control, astrocytes were coincubatedwith LY404039+the PI3K/Akt pathway inhibitor,LY294002 (20 mM), which completely blocked Akt phosphorylationinduced by the mGluR3 agonist (Fig. A)./td
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li style=margin: 0px; padding: 10px 0px; list-style: none; float: left; width: 760px; border-bottom-width: 1px; border-bottom-style: solid; border-bottom-color: rgb(229, 229, 229);a class=proForFlash style=margin: 0px; padding: 0px; color: rgb(52, 84, 140); cursor: pointer;
p class=product_citation_p style=margin: 0px; padding: 0px; float: left; width: 760px;Heterocomplex formation of 5-HT2A-mGlu2 and its relevance for cellular signaling cascades. [Delille HK, et al. Neuropharm 2012;62(7):2184-91]/p
/a/li
li style=margin: 0px; padding: 10px 0px; list-style: none; float: left; width: 760px; border-bottom-width: 1px; border-bottom-style: solid; border-bottom-color: rgb(229, 229, 229);a class=proForFlash style=margin: 0px; padding: 0px; color: rgb(52, 84, 140); cursor: pointer;
p class=product_citation_p style=margin: 0px; padding: 0px; float: left; width: 760px;Reduced cAMP, Akt activation and p65-c-Rel dimerization: mechanisms involved in the protective effects of mGluR3 agonists in cultured astrocytes. [Durand D, et al. PLoS One 2011;6(7):e22235]/p
/a/li
li style=margin: 0px; padding: 10px 0px; list-style: none; float: left; width: 760px; border-bottom-width: 1px; border-bottom-style: solid; border-bottom-color: rgb(229, 229, 229);a class=proForFlash style=margin: 0px; padding: 0px; color: rgb(52, 84, 140); cursor: pointer;
p class=product_citation_p style=margin: 0px; padding: 0px; float: left; width: 760px;Glutamate agonist LY404,039 for treating schizophrenia has afï¬nity for the dopamine D2High receptor. [Seeman P, et al. Synapse 2009;63(10):935-9]/p
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h1 itemprop=name style=margin: 0px 20px 0px 0px; padding: 0px; font-size: 24px; float: left;LY404039/h1
div class=product_c_title style=margin: 0px 20px 0px 0px; padding: 0px; height: 25px; font-size: 12px; float: left;span class=p_title style=margin: 0px 15px 0px 0px; padding: 0px; float: left;Catalog No.S6001/spanspan class=star01 fl style=margin: 2px 0px 0px; padding: 0px; float: left; width: 70px; height: 13px; vertical-align: middle; background-image: url(http://file.selleckchem.com/images/bg.gif); background-position: -200px -70px; background-repeat: no-repeat no-repeat;
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p class=new_title style=margin: 5px 0px 10px; padding: 0px; clear: both; font-size: 11px; line-height: 14.399999618530273px;LY404039 is a potent agonist of recombinant humannbsp;b style=margin: 0px; padding: 0px;mGlu2/mGlu3/bnbsp;receptors withnbsp;b style=margin: 0px; padding: 0px;Kspan style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: 0.25em;i/span/bnbsp;of 149 nM/92 nM, shows gt;100-fold selectivity over ionotropic glutamate receptors, glutamate transporters, and other receptors. Phase 3./p
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td width=80 style=margin: 0px; padding: 3px 8px;USD 88/td
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td width=80 style=margin: 0px; padding: 3px 8px;USD 340/td
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td width=80 style=margin: 0px; padding: 3px 8px;USD 592/td
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h3 id=biologicalActivity style=margin: 25px 0px 0px; padding: 0px; height: 25px; font-size: 14px; font-family: Arial, Tahoma, Helvetica; line-height: 19.200000762939453px;Biological Activity/h3
table width=100% border=0 cellspacing=0 cellpadding=0 class=product_show_table style=margin: 0px; padding: 0px; border-collapse: collapse; border-spacing: 0px; border-style: solid; border-color: rgb(229, 229, 229); color: rgb(0, 0, 0); font-family: Arial, Tahoma, Helvetica; font-size: 12px; line-height: 19.200000762939453px;
tbody style=margin: 0px; padding: 0px;
tr style=margin: 0px; padding: 0px;
th width=16% style=margin: 0px; padding: 5px 0px 5px 15px; font-weight: normal; border-style: solid; border-color: rgb(229, 229, 229);Description/th
td colspan=6 style=margin: 0px; padding: 5px 15px; text-align: justify; border-style: solid; border-color: rgb(229, 229, 229);LY404039 is a potent agonist of recombinant humannbsp;b style=margin: 0px; padding: 0px;mGlu2/mGlu3/bnbsp;receptors withnbsp;b style=margin: 0px; padding: 0px;Kspan style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: 0.25em;i/span/bnbsp;of 149 nM/92 nM, shows gt;100-fold selectivity over ionotropic glutamate receptors, glutamate transporters, and other receptors. Phase 3./td
/tr
tr style=margin: 0px; padding: 0px;
th style=margin: 0px; padding: 5px 0px 5px 15px; font-weight: normal; border-style: solid; border-color: rgb(229, 229, 229);Targets/th
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);Recombinant human mGlu2/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);Recombinant human mGlu3/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);Rat neurons expressing native mGlu2/3/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);nbsp;/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);nbsp;/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);nbsp;/td
/tr
tr style=margin: 0px; padding: 0px;
th style=margin: 0px; padding: 5px 0px 5px 15px; font-weight: normal; border-style: solid; border-color: rgb(229, 229, 229);IC50/th
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);149 nM (Kspan style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: 0.25em;i/span)/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);92 nM (Kspan style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: 0.25em;i/span)/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);88 nM (Kspan style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: 0.25em;i/span)nbsp;span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;a href=http://www.selleckchem.com/products/LY2140023(LY404039).html#s_ref class=sref style=margin: 0px; padding: 0px; text-decoration: none; color: rgb(52, 84, 140); cursor: pointer;[1]/a/span/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);nbsp;/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);nbsp;/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);nbsp;/td
/tr
tr style=margin: 0px; padding: 0px;
th style=margin: 0px; padding: 5px 0px 5px 15px; font-weight: normal; border-style: solid; border-color: rgb(229, 229, 229);i style=margin: 0px; padding: 0px;In vitro/i/th
td colspan=6 style=margin: 0px; padding: 5px 15px; text-align: justify; border-style: solid; border-color: rgb(229, 229, 229);LY404039 exhibits low binding affinity to group III mGlu receptors including mGlu6, mGlu7 and mGlu8 with a Kspan style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: 0.25em;i/spanvalue more than 5 mu;M. LY404039 shows little affinity for ionotropic glutamate receptors, glutamate transporter subtypes, monoamine and other receptors. LY404039 potently inhibits forskolin-stimulated cAMP formation in cells expressing human mGlu2 and mGlu3 receptors. LY404039 suppresses electrically evoked excitatory activity in the striatum, and serotonin-induced L-glutamate release in the prefrontal cortex. LY404039 could modulate glutamatergic activity in limbic and forebrain areas relevant to psychiatric disorders and may be devoid of negative side effects associated with current antipsychotics and anxiolytics.nbsp;span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;a href=http://www.selleckchem.com/products/LY2140023(LY404039).html#s_ref class=sref style=margin: 0px; padding: 0px; text-decoration: none; color: rgb(52, 84, 140); cursor: pointer;[1]/a/span/td
/tr
tr style=margin: 0px; padding: 0px;
th style=margin: 0px; padding: 5px 0px 5px 15px; font-weight: normal; border-style: solid; border-color: rgb(229, 229, 229);i style=margin: 0px; padding: 0px;In vivo/i/th
td colspan=6 style=margin: 0px; padding: 5px 15px; text-align: justify; border-style: solid; border-color: rgb(229, 229, 229);LY404039 demonstrates higher plasma exposure and better oral bioavailability. LY404039 may be valuable in the treatment of neuropsychiatric disorders, including anxiety and psychosis.nbsp;span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;a href=http://www.selleckchem.com/products/LY2140023(LY404039).html#s_ref class=sref style=margin: 0px; padding: 0px; text-decoration: none; color: rgb(52, 84, 140); cursor: pointer;[1]/a/spannbsp;In wild-type animals, LY404039 significantly reverses d-amphetamine(AMP)-induced increase in ambulations, distance traveled, and reduced time spent at rest. LY404039 reverses phencyclidine (PCP)-evoked behaviors at 10 mg/kg. The antipsychotic-like effects of LY404039 on PCP and AMP-evoked behavioral activation are absent in mGlu2 and mGlu2/3 but not in mGlu3 receptor-deficient mice. In contrast, clozapine and risperidone inhibit PCP-evoked behaviors in both wild-type and mGlu2/3 receptor-deficient mice.nbsp;span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;a href=http://www.selleckchem.com/products/LY2140023(LY404039).html#s_ref class=sref style=margin: 0px; padding: 0px; text-decoration: none; color: rgb(52, 84, 140); cursor: pointer;[2]/a/spannbsp;LY404039 reduces responding on the EtOH in the pavlovian spontaneous recovery (PSR) test and reduces the expression of an alcohol deprivation effect (ADE) during relapse, but does not affect EtOH responding under maintenance conditions. LY404039 inhibits the expression of alcohol seeking and relapse behavior without altering alcohol self-administration behavior.nbsp;span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;a href=http://www.selleckchem.com/products/LY2140023(LY404039).html#s_ref class=sref style=margin: 0px; padding: 0px; text-decoration: none; color: rgb(52, 84, 140); cursor: pointer;[3]/a/spanMoreover, LY404039 attenuates amphetamine- and phencyclidine-induced hyperlocomotion. LY404039 could inhibit conditioned avoidance responding and also reduces fear-potentiated startle in rats and marble burying in mice. Importantly, LY404039 does not produce sedative effects or motor impairment in the conditioned avoidance task. LY404039 also increases dopamine and serotonin release/turnover in the prefrontal cortex.nbsp;span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;a href=http://www.selleckchem.com/products/LY2140023(LY404039).html#s_ref class=sref style=margin: 0px; padding: 0px; text-decoration: none; color: rgb(52, 84, 140); cursor: pointer;[4]/a/span/td
/tr
tr style=margin: 0px; padding: 0px;
th style=margin: 0px; padding: 5px 0px 5px 15px; font-weight: normal; border-style: solid; border-color: rgb(229, 229, 229);Features/th
td colspan=6 style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);Under investigation as an exciting new medicine that may herald the arrival of third-generation antipsychotic drugs./td
/tr
/tbody
/table
h3 id=protocol style=margin: 25px 0px 0px; padding: 0px; height: 25px; font-size: 14px; font-family: Arial, Tahoma, Helvetica; line-height: 19.200000762939453px;Protocolspan style=margin: 0px; padding: 0px; font-weight: normal;(Only for Reference)/span/h3
h4 style=margin: 0px; padding: 0px; font-family: Arial, Tahoma, Helvetica; font-size: 12px; line-height: 19.200000762939453px;Kinase Assay:nbsp;span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;a href=http://www.selleckchem.com/products/LY2140023(LY404039).html#s_ref class=sref style=margin: 0px; padding: 0px; text-decoration: none; color: rgb(52, 84, 140); cursor: pointer;[1]/a/span/h4
table width=100% border=0 cellspacing=0 cellpadding=0 class=product_show_table style=margin: 0px; padding: 0px; border-collapse: collapse; border-spacing: 0px; border-style: solid; border-color: rgb(229, 229, 229); color: rgb(0, 0, 0); font-family: Arial, Tahoma, Helvetica; font-size: 12px; line-height: 19.200000762939453px;
tbody style=margin: 0px; padding: 0px;
tr style=margin: 0px; padding: 0px;
th width=16% style=margin: 0px; padding: 5px 0px 5px 15px; font-weight: normal; border-style: solid; border-color: rgb(229, 229, 229);Receptor Binding Assays/th
td style=margin: 0px; padding: 5px 15px; text-align: justify; border-style: solid; border-color: rgb(229, 229, 229);LY404039 is dissolved in DMSO to make a 10 mM stock solution. Cell lines expressing human mGlu2, mGlu3, mGlu1a, mGlu5a, mGlu4a, mGlu6, mGlu7a, and mGlu8 receptors are derived and cultured in DMEM with 5% dialyzed fetal bovine serum, 1 mM glutamine, 1 mM sodium pyruvate, 50 mg/mL Geneticin, and 0.2 mg/mL hygromycin B. Confluent cultures are passaged weekly. These cells are referred to as rat glutamate transporter (RGT) cells. RGT cells are actually AV12-664 cells, which have been stably transfected with a glutamate transporter (GLAST) to prevent the accumulation of L-glutamate in the cell media. Membranes from mGlu receptor-expressing RGT cells are prepared by harvesting adherent cells from confluent T-150 flasks with a cell scraper. Cells and media are then placed in 50-mL conical tubes and centrifuged at 10span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;3/spannbsp;g for 5 min at 4 deg;C. The supernatant is removed, and the pellet is frozen at -10 deg;C until use. Frozen pellets are routinely thawed at room temperature for about 10 min when required. Washed cell membranes are prepared by adding 20 mL of 10 mM potassium phosphate buffer, pH 7.6 and 100 mM potassium bromide, at 5 deg;C and homogenizing with a tissuemizer for 15 s at 90% output. The homogenate is centrifuged at 4.8 times; 10span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;3/spannbsp;g at 5 deg;C for 10 min. This last step is repeated twice, the final pellet is resuspended in 10 mL of the same buffer and reserved on ice until initiating the binding assay. [span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;3/spanH]LY341495 Binding: Group II mGlu Receptors: [span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;3/spanH]LY341495 binding is assayed in a reaction mixture containing 10 mM potassium phosphate, pH 7.6, 100 mM potassium bromide, and 1nM [span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;3/spanH]LY341495 (final volume, 500 mL). The incubation is initiated by the addition of the membrane suspension (15 mg of membrane protein) and kept on ice for 30 min. Incubation is terminated by rapid filtration with a cell harvester through glass fiber Whatman GF/B filters prewet with the same potassium phosphate buffer assay buffer at 4 deg;C. The filters are washed 5 times with 1 mL of buffer. Filter sections are transferred to minivials, and 5 mL liquid scintillation cocktail is added to each vial. Vials are allowed to set for several hours before counting on a liquid scintillation counter. Protein concentrations are quantified by microassay. Nonspecific binding is determined in the presence of 1 mM L-glutamate. [span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;3/spanH]LY341495 Binding: Group III mGlu Receptors: Membranes from cells expressing recombinant human group III mGlu receptors are prepared the same as described for group II mGlu receptor membranes. To start the reaction, washed tissue (0.05ndash;0.20 mg of protein) is added to 10 nM [span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;3/spanH]LY341495 and LY404039 in assay buffer. The final assay volume is 0.5 mL. Nonspecific binding is defined with 1 mM L-glutamate or 1 mM L-serine-O-phosphate (for mGlu7a). Assay plates are incubated for 45 min on ice, and the reaction is terminated by rapid filtration (GF/B filters) and washed twice with 1 mL of ice-cold assay buffer. Filters are placed in minivials, scintillation cocktail is added and counting is done in a liquid scintillation counter. Protein concentration is determined using the microassay. [span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;3/spanH]LY341495 Binding to Rat Brain Membranes: Brain tissue is obtained by decapitating adult male Sprague-Dawley rats (150ndash;250g). The forebrain (cortex, striatum, and hippocampus) is used; the brain tissue is homogenized in 30 mM Tris-HCl buffer, pH 7.6 and 2.5 mM CaClspan style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: 0.25em;2/span, at 5 deg;C and washed 3 times by centrifugation. The material is incubated at 37 deg;C for 30 min followed by 3 more washes, finally resuspended in 10 volumes of buffer and frozen at -20 deg;C. Frozen pellets of rat brain homogenate are thawed on the day of assay and washed 3 times with ice-cold assay buffer (10 mM potassium phosphate containing 100 mM potassium bromide, pH 7.6). The tissue (0.02ndash;0.06 mg of protein) is added to deep-well polypropylene microtiter plates, which contain 1 nM [span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;3/spanH]LY341495 and LY404039 in assay buffer. The final assay volume is 0.5 mL. Nonspecific binding is defined with 1 mM L-glutamate. Assay plates are incubated for 30 minutes on ice, and bound and free radioligands are separated by rapid filtration with 5 times; 1 mL of ice-cold assay buffer using Whatman GF/B filters. Protein concentration is determined using the microassay./td
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/table
h4 style=margin: 0px; padding: 0px; font-family: Arial, Tahoma, Helvetica; font-size: 12px; line-height: 19.200000762939453px;Animal Study:nbsp;span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;a href=http://www.selleckchem.com/products/LY2140023(LY404039).html#s_ref class=sref style=margin: 0px; padding: 0px; text-decoration: none; color: rgb(52, 84, 140); cursor: pointer;[2]/a/span/h4
table width=100% border=0 cellspacing=0 cellpadding=0 class=product_show_table style=margin: 0px; padding: 0px; border-collapse: collapse; border-spacing: 0px; border-style: solid; border-color: rgb(229, 229, 229); color: rgb(0, 0, 0); font-family: Arial, Tahoma, Helvetica; font-size: 12px; line-height: 19.200000762939453px;
tbody style=margin: 0px; padding: 0px;
tr style=margin: 0px; padding: 0px;
th width=16% style=margin: 0px; padding: 5px 0px 5px 15px; font-weight: normal; border-style: solid; border-color: rgb(229, 229, 229);Animal Models/th
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);Separate mGlu2 and mGlu3 receptor knockout mice are established./td
/tr
tr style=margin: 0px; padding: 0px;
th width=16% style=margin: 0px; padding: 5px 0px 5px 15px; font-weight: normal; border-style: solid; border-color: rgb(229, 229, 229);Dosages/th
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);10 mg/kg/td
/tr
tr style=margin: 0px; padding: 0px;
th width=16% style=margin: 0px; padding: 5px 0px 5px 15px; font-weight: normal; border-style: solid; border-color: rgb(229, 229, 229);Administration/th
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);Administered via i.p./td
/tr
tr style=margin: 0px; padding: 0px;
th width=16% style=margin: 0px; padding: 5px 0px 5px 15px; font-weight: normal; border-style: solid; border-color: rgb(229, 229, 229);Solubility/th
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);30% propylene glycol, 5% Tween 80, 65% D5W, 30 mg/mL/td
/tr
/tbody
/table
pa id=s_ref style=margin: 0px; padding: 0px; color: rgb(52, 84, 140); cursor: pointer; font-family: Arial, Tahoma, Helvetica; line-height: 19.200000762939453px; clear: both; float: left; height: 0px; font-size: 0px;1/a/p
h4 class=reference margin_t style=margin: 10px 0px 0px; padding: 0px; font-family: Arial, Tahoma, Helvetica; font-size: 12px; line-height: 19.200000762939453px;References/h4
h3 id=clinical style=margin: 25px 0px 0px; padding: 0px; height: 25px; font-size: 14px; font-family: Arial, Tahoma, Helvetica; line-height: 19.200000762939453px;Clinical Trial Informationspan class=inpo style=margin: 0px 0px 0px 10px; padding: 0px; font-size: 12px; font-weight: normal;( data from http://clinicaltrials.gov)/span/h3
table width=100% border=0 cellspacing=0 cellpadding=0 class=inpo_table style=margin: 0px; padding: 0px; border-collapse: collapse; border-spacing: 0px; border-style: solid; border-color: rgb(229, 229, 229); color: rgb(0, 0, 0); font-family: Arial, Tahoma, Helvetica; font-size: 12px; line-height: 19.200000762939453px;
tbody style=margin: 0px; padding: 0px;
tr style=margin: 0px; padding: 0px;
th width=15% style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229); background-color: rgb(249, 249, 249);NCT Number/th
th width=12% style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229); background-color: rgb(249, 249, 249);Recruitment/th
th width=35% style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229); background-color: rgb(249, 249, 249);Conditions/th
th width=19% style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229); background-color: rgb(249, 249, 249);Sponsorbr style=margin: 0px; padding: 0px; /
/Collaborators/th
th width=10% style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229); background-color: rgb(249, 249, 249);Start Date/th
th width=9% style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229); background-color: rgb(249, 249, 249);Phases/th
/tr
tr style=margin: 0px; padding: 0px;
td style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229);NCT01475136/td
td style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229);Completed/td
td style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229);Hepatic Insufficiency/td
td style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229);Eli Lilly and Company/td
td style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229);2011-11/td
td style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229);Phase 1/td
/tr
tr style=margin: 0px; padding: 0px;
td style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229);NCT01591330/td
td style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229);Completed/td
td style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229);Healthy Volunteers/td
td style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229);Eli Lilly and Company/td
td style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229);2012-04/td
td style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229);Phase 1/td
/tr
tr style=margin: 0px; padding: 0px;
td style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229);NCT01609218/td
td style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229);Completed/td
td style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229);Healthy Volunteer Study/td
td style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229);Eli Lilly and Company/td
td style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229);2012-05/td
td style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229);Phase 1/td
/tr
tr style=margin: 0px; padding: 0px;
td style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229);NCT01637142/td
td style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229);Completed/td
td style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229);Healthy Participants/td
td style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229);Eli Lilly and Company/td
td style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229);2012-07/td
td style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229);Phase 1/td
/tr
tr style=margin: 0px; padding: 0px;
td style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229);NCT01659177/td
td style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229);Withdrawn/td
td style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229);Healthy Participants/td
td style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229);Eli Lilly and Company/td
td style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229);2012-08/td
td style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229);Phase 1/td
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h3 id=chemicalInformation style=margin: 25px 0px 0px; padding: 0px; height: 25px; font-size: 14px; font-family: Arial, Tahoma, Helvetica; line-height: 19.200000762939453px;Chemical Information/h3
pa href=http://file.selleckchem.com/downloads/product-sdf/ly2140023-ly404039-s6001.SDF style=margin: -25px 0px 0px 180px; padding: 0px; text-decoration: none; color: rgb(52, 84, 140); cursor: pointer; font-family: Arial, Tahoma, Helvetica; font-size: 12px; line-height: 19.200000762939453px; float: left;Download LY404039 SDF/a/p
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table width=100% border=0 cellspacing=0 cellpadding=0 class=show_tab01 fl style=margin: 0px 0px 10px; padding: 0px; border-collapse: collapse; border-spacing: 0px; width: 375px; float: left;
tbody style=margin: 0px; padding: 0px;
tr style=margin: 0px; padding: 0px;
th width=45% style=margin: 0px; padding: 5px 0px 5px 15px; font-weight: normal; border-style: solid; border-color: rgb(229, 229, 229);Molecular Weight (MW)/th
td width=55% style=margin: 0px; padding: 5px 0px 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);235.22/td
/tr
tr style=margin: 0px; padding: 0px;
th width=45% style=margin: 0px; padding: 5px 0px 5px 15px; font-weight: normal; border-style: solid; border-color: rgb(229, 229, 229);Formula/th
td style=margin: 0px; padding: 5px 0px 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);
p style=margin: 0px; padding: 0px;Cspan style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: 0.25em;7/spanHspan style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: 0.25em;9/spanNOspan style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: 0.25em;6/spanS/p
/td
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tr style=margin: 0px; padding: 0px;
th width=45% style=margin: 0px; padding: 5px 0px 5px 15px; font-weight: normal; border-style: solid; border-color: rgb(229, 229, 229);CAS No./th
td style=margin: 0px; padding: 5px 0px 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);635318-11-5/td
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/tbody
/table
table width=100% border=0 cellspacing=0 cellpadding=0 class=show_tab fr style=margin: 0px 0px 10px; padding: 0px; border-collapse: collapse; border-spacing: 0px; width: 375px; float: right;
tbody style=margin: 0px; padding: 0px;
tr style=margin: 0px; padding: 0px;
th rowspan=2 valign=top class=padding5 style=margin: 0px; padding: 5px 0px 5px 10px; font-weight: normal; border-style: solid; border-color: rgb(229, 229, 229);Storage/th
td class=padding5 style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229);3 yearsnbsp;span class=margin_l style=margin: 0px 0px 0px 10px; padding: 0px;-20℃/spanspan class=margin_l style=margin: 0px 0px 0px 10px; padding: 0px;Powder/span/td
/tr
tr style=margin: 0px; padding: 0px;
td class=padding5 style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229);6 monthsspan class=margin_l style=margin: 0px 0px 0px 10px; padding: 0px;-80℃/spanspan class=margin_l style=margin: 0px 0px 0px 10px; padding: 0px;in DMSO/span/td
/tr
tr style=margin: 0px; padding: 0px;
th width=161 valign=top class=padding5 style=margin: 0px; padding: 5px 0px 5px 10px; font-weight: normal; border-style: solid; border-color: rgb(229, 229, 229);Syonnyms/th
td width=214 class=padding5 style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229);N/A/td
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table width=100% border=0 cellspacing=0 cellpadding=0 class=product_show_table mb15 style=margin: 0px 0px 15px; padding: 0px; border-collapse: collapse; border-spacing: 0px; border-style: solid; border-color: rgb(229, 229, 229);
tbody style=margin: 0px; padding: 0px;
tr style=margin: 0px; padding: 0px;
th width=12% rowspan=4 style=margin: 0px; padding: 5px 0px 5px 15px; font-weight: normal; border-style: solid; border-color: rgb(229, 229, 229);strong style=margin: 0px; padding: 0px;Solubility (25deg;C)nbsp;/strongspan class=red style=margin: 0px; padding: 0px; color: rgb(255, 0, 0);*/span/th
td width=10% rowspan=3 class=italic style=margin: 0px; padding: 5px 15px; font-style: italic; border-style: solid; border-color: rgb(229, 229, 229);In vitro/td
td width=50% style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);DMSO/td
td width=28% style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);1 mg/mL (4 mM)/td
/tr
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td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);Water/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);lt;1 mg/mL (lt;1 mM)/td
/tr
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td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);Ethanol/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);lt;1 mg/mL (lt;1 mM)/td
/tr
tr style=margin: 0px; padding: 0px;
td class=italic style=margin: 0px; padding: 5px 15px; font-style: italic; border-style: solid; border-color: rgb(229, 229, 229);In vivo/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);30% propylene glycol, 5% Tween 80, 65% D5W,/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);30 mg/mL/td
/tr
tr style=margin: 0px; padding: 0px;
td colspan=4 style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);span class=red style=margin: 0px; padding: 0px; color: rgb(255, 0, 0);*/spannbsp;lt;1 mg/ml means slightly soluble or insoluble.br style=margin: 0px; padding: 0px; /
span class=red style=margin: 0px; padding: 0px; color: rgb(255, 0, 0);*/spannbsp;Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations./td
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/div
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tr style=margin: 0px; padding: 0px;
th width=153px style=margin: 0px; padding: 5px 0px 5px 15px; font-weight: normal; border-style: solid; border-color: rgb(229, 229, 229);Chemical Name/th
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);(1R,4S,5S,6S)-4-[[(2S)-2-Amino-4-(methylthio)-1-oxobutyl]amino]-2-thiabicyclo[3.1.0]hexane-4,6-dicarboxylic acid 2,2-dioxide/td
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td width=21% style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);Rating/td
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td class=italic style=margin: 0px; padding: 5px 15px; font-style: italic; border-style: solid; border-color: rgb(229, 229, 229);PLoS One, 2011, 6(7), e22235.span style=margin: 0px; padding: 0px; font-style: normal;nbsp;LY404039 purchased from Selleck/span/td
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td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);Method/td
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/tr
tr style=margin: 0px; padding: 0px;
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);Cell Lines/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);astrocytes/td
/tr
tr style=margin: 0px; padding: 0px;
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);Concentrations/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);100 uM/td
/tr
tr style=margin: 0px; padding: 0px;
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);Incubation Time/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);30 min/td
/tr
tr style=margin: 0px; padding: 0px;
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);Results/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);LY404039 also induced Akt phosphorylation per se(Fig. A and B). As a negative control, astrocytes were coincubatedwith LY404039+the PI3K/Akt pathway inhibitor,LY294002 (20 mM), which completely blocked Akt phosphorylationinduced by the mGluR3 agonist (Fig. A)./td
/tr
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p class=product_citation_p style=margin: 0px; padding: 0px; float: left; width: 760px;Heterocomplex formation of 5-HT2A-mGlu2 and its relevance for cellular signaling cascades. [Delille HK, et al. Neuropharm 2012;62(7):2184-91]/p
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p class=product_citation_p style=margin: 0px; padding: 0px; float: left; width: 760px;Reduced cAMP, Akt activation and p65-c-Rel dimerization: mechanisms involved in the protective effects of mGluR3 agonists in cultured astrocytes. [Durand D, et al. PLoS One 2011;6(7):e22235]/p
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li style=margin: 0px; padding: 10px 0px; list-style: none; float: left; width: 760px; border-bottom-width: 1px; border-bottom-style: solid; border-bottom-color: rgb(229, 229, 229);a class=proForFlash style=margin: 0px; padding: 0px; color: rgb(52, 84, 140); cursor: pointer;
p class=product_citation_p style=margin: 0px; padding: 0px; float: left; width: 760px;Glutamate agonist LY404,039 for treating schizophrenia has afï¬nity for the dopamine D2High receptor. [Seeman P, et al. Synapse 2009;63(10):935-9]/p
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