Antibodies
CTEP (RO4956371)
- 貨號 Cat. No.
- S2861
- 規格 Size
- 5~200mg
- 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;CTEP (RO4956371)/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.S2861/span/div
p class=new_title style=margin: 5px 0px 10px; padding: 0px; clear: both; font-size: 11px; line-height: 14.399999618530273px;CTEP is a novel, long-acting, orally bioavailable allosteric antagonist ofnbsp;b style=margin: 0px; padding: 0px;mGlu5/bnbsp;receptor withnbsp;b style=margin: 0px; padding: 0px;IC50/bnbsp;of 2.2 nM, shows gt;1000-fold selectivity over other mGlu receptors./p
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td width=139 style=margin: 0px; padding: 3px 8px;label style=margin: 0px; padding: 0px;10mM/1mL/labelspan class=in_bg style=margin: 0px 0px 0px 4px; padding: 0px 3px; background-color: rgb(255, 120, 0); color: rgb(255, 255, 255); font-size: 11px; background-position: initial initial; background-repeat: initial initial;In DMSO/span/td
td width=80 style=margin: 0px; padding: 3px 8px;USD 529/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;5mg/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=139 style=margin: 0px; padding: 3px 8px;label style=margin: 0px; padding: 0px;10mg/label/td
td width=80 style=margin: 0px; padding: 3px 8px;USD 466/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;50mg/label/td
td width=80 style=margin: 0px; padding: 3px 8px;USD 1348/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;200mg/label/td
td width=80 style=margin: 0px; padding: 3px 8px;USD 3112/td
td width=62 style=margin: 0px; padding: 3px 8px;In stock/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);CTEP is a novel, long-acting, orally bioavailable allosteric antagonist ofnbsp;b style=margin: 0px; padding: 0px;mGlu5/bnbsp;receptor withnbsp;b style=margin: 0px; padding: 0px;IC50/bnbsp;of 2.2 nM, shows gt;1000-fold selectivity over other mGlu receptors./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);mGlu5/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
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);2.2 nMnbsp;span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;a href=http://www.selleckchem.com/products/ctep.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
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);CTEP inhibits quisqualate-induced Caspan style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;2+/spannbsp;mobilization with an IC50 of 11.4 nM and [span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;3/spanH]IP accumulation with an IC50 of 6.4 nM in HEK293 cells stably expressing human mGlu5. CTEP inhibits the constitutive activity of human mGlu5 by approximately 50% with an IC50 of 40.1 nM in HEK293 cells stably expressing human mGlu5.span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;a href=http://www.selleckchem.com/products/ctep.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);CTEP is significantly active at doses of 0.1 mg/kg and 0.3 mg/kg in treatment of anxiety in mouse. CTEP significantly increases drinking time at doses of 0.3 mg/kg and 1.0 mg/kg in the Vogel conflict drinking test in rat, whereas it has no effect at lower doses. The half-life of CTEP (oral) is 18 h, and the B/P ratio based on total drug concentrations in plasma and whole brain homogenates is 2.6 in mice. After single oral doses of 4.5 and 8.7 mg/kg CTEP formulated as microsuspension in a saline/Tween vehicle administrated to adult C57BL/6 mice is rapidly absorbed and achieves close to maximal exposure after approximately 30 min. Chronic administration in adult mice with a dose of 2 mg/kg p.o. every 48 h for 2 months reaches a minimal CTEP brain exposure of 240 ng/g. CTEP fully displaces [span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;3/spanH]ABP688 in mouse brain regions known to express mGlu5, and 50% displacement is achieved with doses producing an average compound concentration of 77.5 ng/g measured in whole brain homogenate.nbsp;span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;a href=http://www.selleckchem.com/products/ctep.html#s_ref class=sref style=margin: 0px; padding: 0px; text-decoration: none; color: rgb(52, 84, 140); cursor: pointer;[1]/a/spannbsp;CTEP (2 mg/kg p.o. bid) achieves uninterrupted mGlu5 occupancy per 48 hours in mice. CTEP (2 mg/kg p.o.) treatment corrects elevated hippocampal long-term depression, excessive protein synthesis, and audiogenic seizures in the Fmr1 knockout mouse.nbsp;span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;a href=http://www.selleckchem.com/products/ctep.html#s_ref class=sref style=margin: 0px; padding: 0px; text-decoration: none; color: rgb(52, 84, 140); cursor: pointer;[2]/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);nbsp;/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/ctep.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);Radioligand Binding Assays/th
td style=margin: 0px; padding: 5px 15px; text-align: justify; border-style: solid; border-color: rgb(229, 229, 229);For all filtration radioligand binding assays, membrane preparations expressing the target receptors or receptor combinations are resuspended in radioligand binding buffer (15 mM Tris-HCl, 120 mM NaCl, 5 mM KCl, 1.25 mM CaClspan style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: 0.25em;2/span, and 1.25 mM MgClspan style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: 0.25em;2/span, pH 7.4), and the membrane suspension is mixed with the appropriate concentrations of radioligand and nonlabeled drugs in 96-well plates in a total volume of 200 mu;L and incubated for 60 min at the appropriate temperature. At the end of the incubation, membranes are filtered onto Whatman Unifilter preincubated with 0.1% polyethyleneimine in wash buffer (50 mM Tris-HCl, pH 7.4) with a Filtermate 196 harvester and washed three times with ice-cold wash buffer. Radioactivity captured on the filter is quantified on a Topcount microplate scintillation counter with quenching correction after the addition of 45 mu;L of MicroScint 40 per well and shaking for 20 min. The concentration of membranes and incubation time is determined for each assay in pilot experiments./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/ctep.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);Animal Models/th
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);Male Sprague-Dawley rats/td
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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);Dosages/th
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);1.0 mg/kg/td
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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);Administration/th
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);orally/td
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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);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, 6 mg/mL/td
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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
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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);NCT01322802/td
td style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229);Recruiting/td
td style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229);Stage III Ovarian Epithelial Cancer|Stage III Ovarian Germ Cell Tumor|Stage IV Ovarian Epithelial Cancer|Stage IV Ovarian Germ Cell Tumor/td
td style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229);FredHutchinsonCancerResearchCenter|Fred Hutchinson Cancer Research Center/University of Washington Cancer Consortium|NationalCancerInstitute(NCI)/td
td style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229);2012-03/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);NCT01536067/td
td style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229);Recruiting/td
td style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229);Waldenstræžšm Macroglobulinemia/td
td style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229);RoswellParkCancerInstitute|NationalCancerInstitute(NCI)/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 2/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);NCT01606241/td
td style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229);Recruiting/td
td style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229);Recurrent Breast Cancer|Recurrent Fallopian Tube Cancer|Recurrent Ovarian Epithelial Cancer|Recurrent Ovarian Germ Cell Tumor|Recurrent Primary Peritoneal Cavity Cancer etc./td
td style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229);MayoClinic/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);NCT01632332/td
td style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229);Recruiting/td
td style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229);HER2-positive Breast Cancer|Male Breast Cancer|Stage II Breast Cancer|Stage IIIA Breast Cancer|Stage IIIB Breast Cancer|Stage IIIC Breast Cancer/td
td style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229);MayoClinic|TapImmune,Inc./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);NCT01729884/td
td style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229);Recruiting/td
td style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229);HER2-positive Breast Cancer|Male Breast Cancer|Recurrent Breast Cancer|Stage IV Breast Cancer/td
td style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229);FredHutchinsonCancerResearchCenter|Fred Hutchinson Cancer Research Center/University of Washington Cancer Consortium|NationalCancerInstitute(NCI)/td
td style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229);2012-12/td
td style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229);Phase 2/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/ctep-s2861.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 CTEP (RO4956371) SDF/a/p
div class=clear-both style=margin: 0px; padding: 0px; clear: both; height: 0px; overflow: hidden; font-family: Arial, Tahoma, Helvetica; font-size: 12px; line-height: 19.200000762939453px;nbsp;/div
div class=clear style=margin: 0px; padding: 0px; zoom: 1; font-family: Arial, Tahoma, Helvetica; font-size: 12px; line-height: 19.200000762939453px;
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);391.77/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;19/spanHspan style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: 0.25em;13/spanClFspan style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: 0.25em;3/spanNspan style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: 0.25em;3/spanO/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);871362-31-1/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);nbsp;/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);78 mg/mL (199 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);10 mg/mL (25 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);6 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
/div
div style=margin: 0px; padding: 0px; font-family: Arial, Tahoma, Helvetica; font-size: 12px; line-height: 19.200000762939453px; height: 10px;nbsp;/div
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=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);Pyridine, 2-chloro-4-[2-[2,5-dimethyl-1-[4-(trifluoromethoxy)phenyl]-1H-imidazol-4-yl]ethynyl]-/td
/tr
/tbody
/table
div class=clear-both style=margin: 0px; padding: 0px; clear: both; height: 0px; overflow: hidden; font-family: Arial, Tahoma, Helvetica; font-size: 12px; line-height: 19.200000762939453px;nbsp;/div
h3 id=chemicalInformation style=margin: 25px 0px 0px; padding: 0px; height: 25px; font-size: 14px; font-family: Arial, Tahoma, Helvetica; line-height: 19.200000762939453px;Preparing Stock Solutions/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=153px style=margin: 0px; padding: 5px 0px 5px 15px; font-weight: normal; border-style: solid; border-color: rgb(229, 229, 229);Stock Solution (1ml DMSO)/th
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);1mM/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);10mM/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);20mM/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);30mM/td
/tr
tr style=margin: 0px; padding: 0px;
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);Mass(mg)/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);0.39177/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);3.9177/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);7.8354/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);11.7531/td
/tr
/tbody
/table
div class=counter style=margin: 10px 0px 0px; padding: 0px; font-size: 14px; font-weight: bold; font-family: Arial, Tahoma, Helvetica; line-height: 19.200000762939453px;a href=http://www.selleckchem.com/molaritycalculator.jsp style=margin: 0px 5px 0px 0px; padding: 5px 15px; text-decoration: none; color: rgb(52, 84, 140); cursor: pointer; display: inline-block; background-color: rgb(255, 239, 187); border: 1px solid rgb(237, 218, 159); background-position: initial initial; background-repeat: initial initial;Molarity Calculator/anbsp;a href=http://www.selleckchem.com/dilutioncalculator.jsp style=margin: 0px 5px 0px 0px; padding: 5px 15px; text-decoration: none; color: rgb(52, 84, 140); cursor: pointer; display: inline-block; background-color: rgb(255, 239, 187); border: 1px solid rgb(237, 218, 159); background-position: initial initial; background-repeat: initial initial;Dilution Calculator/anbsp;a href=http://www.selleckchem.com/molecular-weight-calculator.html style=margin: 0px 5px 0px 0px; padding: 5px 15px; text-decoration: none; color: rgb(52, 84, 140); cursor: pointer; display: inline-block; background-color: rgb(255, 239, 187); border: 1px solid rgb(237, 218, 159); background-position: initial initial; background-repeat: initial initial;Molecular Weight Calculator/a/div
pnbsp;/p
pnbsp;/p
pnbsp;/p
h1 itemprop=name style=margin: 0px 20px 0px 0px; padding: 0px; font-size: 24px; float: left;CTEP (RO4956371)/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.S2861/span/div
p class=new_title style=margin: 5px 0px 10px; padding: 0px; clear: both; font-size: 11px; line-height: 14.399999618530273px;CTEP is a novel, long-acting, orally bioavailable allosteric antagonist ofnbsp;b style=margin: 0px; padding: 0px;mGlu5/bnbsp;receptor withnbsp;b style=margin: 0px; padding: 0px;IC50/bnbsp;of 2.2 nM, shows gt;1000-fold selectivity over other mGlu receptors./p
/div
form id=prodaddfrom action=http://www.selleckchem.com/cart/addCart.jhtml method=post name=sizelist style=margin: 0px; padding: 0px; font-family: Arial, Tahoma, Helvetica; font-size: 12px; line-height: 19.200000762939453px;
div class=product_record id=selectTotal style=margin: 0px; padding: 0px; background-color: rgb(245, 245, 245); background-position: initial initial; background-repeat: initial initial;
table border=0 cellspacing=0 cellpadding=0 style=margin: 0px; padding: 0px; border-collapse: collapse; border-spacing: 0px; width: 760px;
tbody style=margin: 0px; padding: 0px;
tr style=margin: 0px; padding: 0px;
th width=153 style=margin: 0px; padding: 0px 0px 0px 15px; line-height: 14px; font-size: 14px; border-bottom-style: solid; border-bottom-color: rgb(211, 217, 225); background-color: rgb(221, 228, 236);label style=margin: 0px; padding: 0px;Size/label/th
th width=76 style=margin: 0px; padding: 8px; line-height: 14px; font-size: 14px; border-bottom-style: solid; border-bottom-color: rgb(211, 217, 225); background-color: rgb(221, 228, 236);Price/th
th width=55 style=margin: 0px; padding: 8px; line-height: 14px; font-size: 14px; border-bottom-style: solid; border-bottom-color: rgb(211, 217, 225); background-color: rgb(221, 228, 236);Stock/th
th width=74 style=margin: 0px; padding: 8px; line-height: 14px; font-size: 14px; border-bottom-style: solid; border-bottom-color: rgb(211, 217, 225); background-color: rgb(221, 228, 236);Quantity/th
th width=402 style=margin: 0px; padding: 8px; line-height: 14px; font-size: 14px; border-bottom-style: solid; border-bottom-color: rgb(211, 217, 225); background-color: rgb(221, 228, 236);nbsp;/th
/tr
tr style=margin: 0px; padding: 0px;
td colspan=4 valign=top class=pt style=margin: 0px; padding: 3px 8px;
table width=91% border=0 cellspacing=0 cellpadding=0 style=margin: 0px; padding: 0px; border-collapse: collapse; border-spacing: 0px; width: 374px;
tbody style=margin: 0px; padding: 0px;
tr style=margin: 0px; padding: 0px;
td width=139 style=margin: 0px; padding: 3px 8px;label style=margin: 0px; padding: 0px;10mM/1mL/labelspan class=in_bg style=margin: 0px 0px 0px 4px; padding: 0px 3px; background-color: rgb(255, 120, 0); color: rgb(255, 255, 255); font-size: 11px; background-position: initial initial; background-repeat: initial initial;In DMSO/span/td
td width=80 style=margin: 0px; padding: 3px 8px;USD 529/td
td width=62 style=margin: 0px; padding: 3px 8px;In stock/td
td width=61 style=margin: 0px; padding: 3px 8px;select name=cartDTOs[2].quantity style=margin: 0px; padding: 0px; border-color: rgb(171, 171, 171); width: 40px;nbsp;
option value=0 style=margin: 0px; padding: 0px;0/option
nbsp;
option value=1 style=margin: 0px; padding: 0px;1/option
nbsp;
option value=2 style=margin: 0px; padding: 0px;2/option
nbsp;
option value=3 style=margin: 0px; padding: 0px;3/option
nbsp;
option value=4 style=margin: 0px; padding: 0px;4/option
nbsp;
option value=5 style=margin: 0px; padding: 0px;5/option
nbsp;
option value=6 style=margin: 0px; padding: 0px;6/option
nbsp;
option value=7 style=margin: 0px; padding: 0px;7/option
nbsp;
option value=8 style=margin: 0px; padding: 0px;8/option
nbsp;
option value=9 style=margin: 0px; padding: 0px;9/option
nbsp;
option value=10 style=margin: 0px; padding: 0px;10/option
nbsp;/select/td
/tr
tr style=margin: 0px; padding: 0px;
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 340/td
td width=62 style=margin: 0px; padding: 3px 8px;In stock/td
td width=61 style=margin: 0px; padding: 3px 8px;select name=cartDTOs[0].quantity style=margin: 0px; padding: 0px; border-color: rgb(171, 171, 171); width: 40px;nbsp;
option value=0 style=margin: 0px; padding: 0px;0/option
nbsp;
option value=1 style=margin: 0px; padding: 0px;1/option
nbsp;
option value=2 style=margin: 0px; padding: 0px;2/option
nbsp;
option value=3 style=margin: 0px; padding: 0px;3/option
nbsp;
option value=4 style=margin: 0px; padding: 0px;4/option
nbsp;
option value=5 style=margin: 0px; padding: 0px;5/option
nbsp;
option value=6 style=margin: 0px; padding: 0px;6/option
nbsp;
option value=7 style=margin: 0px; padding: 0px;7/option
nbsp;
option value=8 style=margin: 0px; padding: 0px;8/option
nbsp;
option value=9 style=margin: 0px; padding: 0px;9/option
nbsp;
option value=10 style=margin: 0px; padding: 0px;10/option
nbsp;/select/td
/tr
tr style=margin: 0px; padding: 0px;
td width=139 style=margin: 0px; padding: 3px 8px;label style=margin: 0px; padding: 0px;10mg/label/td
td width=80 style=margin: 0px; padding: 3px 8px;USD 466/td
td width=62 style=margin: 0px; padding: 3px 8px;In stock/td
td width=61 style=margin: 0px; padding: 3px 8px;select name=cartDTOs[1].quantity style=margin: 0px; padding: 0px; border-color: rgb(171, 171, 171); width: 40px;nbsp;
option value=0 style=margin: 0px; padding: 0px;0/option
nbsp;
option value=1 style=margin: 0px; padding: 0px;1/option
nbsp;
option value=2 style=margin: 0px; padding: 0px;2/option
nbsp;
option value=3 style=margin: 0px; padding: 0px;3/option
nbsp;
option value=4 style=margin: 0px; padding: 0px;4/option
nbsp;
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td width=139 style=margin: 0px; padding: 3px 8px;label style=margin: 0px; padding: 0px;50mg/label/td
td width=80 style=margin: 0px; padding: 3px 8px;USD 1348/td
td width=62 style=margin: 0px; padding: 3px 8px;In stock/td
td width=61 style=margin: 0px; padding: 3px 8px;select name=cartDTOs[3].quantity style=margin: 0px; padding: 0px; border-color: rgb(171, 171, 171); width: 40px;nbsp;
option value=0 style=margin: 0px; padding: 0px;0/option
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td width=139 style=margin: 0px; padding: 3px 8px;label style=margin: 0px; padding: 0px;200mg/label/td
td width=80 style=margin: 0px; padding: 3px 8px;USD 3112/td
td width=62 style=margin: 0px; padding: 3px 8px;In stock/td
td width=61 style=margin: 0px; padding: 3px 8px;select name=cartDTOs[4].quantity style=margin: 0px; padding: 0px; border-color: rgb(171, 171, 171); width: 40px;nbsp;
option value=0 style=margin: 0px; padding: 0px;0/option
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pnbsp;img class=flag_ico src=http://file.selleckchem.com/images/flag/taiwan.png style=font-size: 12px; margin: 0px 3px 0px 0px; padding: 0px; border: none; display: inline-block; width: 20px; height: 20px; vertical-align: middle; font-family: Arial, Tahoma, Helvetica; line-height: 19.200000762939453px; background-color: rgb(245, 245, 245); alt= /strong style=font-size: 12px; margin: 0px; padding: 0px; font-family: Arial, Tahoma, Helvetica; line-height: 19.200000762939453px; background-color: rgb(245, 245, 245);Distributor/strongspan style=font-size: 12px; font-family: Arial, Tahoma, Helvetica; line-height: 19.200000762939453px; background-color: rgb(245, 245, 245);nbsp;/spanspan class=font11 margin_l style=font-size: 12px; margin: 0px 0px 0px 10px; padding: 0px; font-family: Arial, Tahoma, Helvetica; line-height: 19.200000762939453px; background-color: rgb(245, 245, 245);Tel: +886-2-2827-1197span class=margin_l style=margin: 0px 0px 0px 10px; padding: 0px;a href=mailto:jimmy@new.abscience.com.tw rel=nofollow style=margin: 0px; padding: 0px; text-decoration: none; color: rgb(52, 84, 140); cursor: pointer;jimmy@new.abscience.com.tw/a/span/span/p
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);CTEP is a novel, long-acting, orally bioavailable allosteric antagonist ofnbsp;b style=margin: 0px; padding: 0px;mGlu5/bnbsp;receptor withnbsp;b style=margin: 0px; padding: 0px;IC50/bnbsp;of 2.2 nM, shows gt;1000-fold selectivity over other mGlu receptors./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);mGlu5/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
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);2.2 nMnbsp;span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;a href=http://www.selleckchem.com/products/ctep.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
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);CTEP inhibits quisqualate-induced Caspan style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;2+/spannbsp;mobilization with an IC50 of 11.4 nM and [span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;3/spanH]IP accumulation with an IC50 of 6.4 nM in HEK293 cells stably expressing human mGlu5. CTEP inhibits the constitutive activity of human mGlu5 by approximately 50% with an IC50 of 40.1 nM in HEK293 cells stably expressing human mGlu5.span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;a href=http://www.selleckchem.com/products/ctep.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);CTEP is significantly active at doses of 0.1 mg/kg and 0.3 mg/kg in treatment of anxiety in mouse. CTEP significantly increases drinking time at doses of 0.3 mg/kg and 1.0 mg/kg in the Vogel conflict drinking test in rat, whereas it has no effect at lower doses. The half-life of CTEP (oral) is 18 h, and the B/P ratio based on total drug concentrations in plasma and whole brain homogenates is 2.6 in mice. After single oral doses of 4.5 and 8.7 mg/kg CTEP formulated as microsuspension in a saline/Tween vehicle administrated to adult C57BL/6 mice is rapidly absorbed and achieves close to maximal exposure after approximately 30 min. Chronic administration in adult mice with a dose of 2 mg/kg p.o. every 48 h for 2 months reaches a minimal CTEP brain exposure of 240 ng/g. CTEP fully displaces [span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;3/spanH]ABP688 in mouse brain regions known to express mGlu5, and 50% displacement is achieved with doses producing an average compound concentration of 77.5 ng/g measured in whole brain homogenate.nbsp;span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;a href=http://www.selleckchem.com/products/ctep.html#s_ref class=sref style=margin: 0px; padding: 0px; text-decoration: none; color: rgb(52, 84, 140); cursor: pointer;[1]/a/spannbsp;CTEP (2 mg/kg p.o. bid) achieves uninterrupted mGlu5 occupancy per 48 hours in mice. CTEP (2 mg/kg p.o.) treatment corrects elevated hippocampal long-term depression, excessive protein synthesis, and audiogenic seizures in the Fmr1 knockout mouse.nbsp;span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;a href=http://www.selleckchem.com/products/ctep.html#s_ref class=sref style=margin: 0px; padding: 0px; text-decoration: none; color: rgb(52, 84, 140); cursor: pointer;[2]/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);nbsp;/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/ctep.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);Radioligand Binding Assays/th
td style=margin: 0px; padding: 5px 15px; text-align: justify; border-style: solid; border-color: rgb(229, 229, 229);For all filtration radioligand binding assays, membrane preparations expressing the target receptors or receptor combinations are resuspended in radioligand binding buffer (15 mM Tris-HCl, 120 mM NaCl, 5 mM KCl, 1.25 mM CaClspan style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: 0.25em;2/span, and 1.25 mM MgClspan style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: 0.25em;2/span, pH 7.4), and the membrane suspension is mixed with the appropriate concentrations of radioligand and nonlabeled drugs in 96-well plates in a total volume of 200 mu;L and incubated for 60 min at the appropriate temperature. At the end of the incubation, membranes are filtered onto Whatman Unifilter preincubated with 0.1% polyethyleneimine in wash buffer (50 mM Tris-HCl, pH 7.4) with a Filtermate 196 harvester and washed three times with ice-cold wash buffer. Radioactivity captured on the filter is quantified on a Topcount microplate scintillation counter with quenching correction after the addition of 45 mu;L of MicroScint 40 per well and shaking for 20 min. The concentration of membranes and incubation time is determined for each assay in pilot experiments./td
/tr
/tbody
/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/ctep.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);Animal Models/th
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);Male Sprague-Dawley rats/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);1.0 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);orally/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, 6 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);NCT01322802/td
td style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229);Recruiting/td
td style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229);Stage III Ovarian Epithelial Cancer|Stage III Ovarian Germ Cell Tumor|Stage IV Ovarian Epithelial Cancer|Stage IV Ovarian Germ Cell Tumor/td
td style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229);FredHutchinsonCancerResearchCenter|Fred Hutchinson Cancer Research Center/University of Washington Cancer Consortium|NationalCancerInstitute(NCI)/td
td style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229);2012-03/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);NCT01536067/td
td style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229);Recruiting/td
td style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229);Waldenstræžšm Macroglobulinemia/td
td style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229);RoswellParkCancerInstitute|NationalCancerInstitute(NCI)/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 2/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);NCT01606241/td
td style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229);Recruiting/td
td style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229);Recurrent Breast Cancer|Recurrent Fallopian Tube Cancer|Recurrent Ovarian Epithelial Cancer|Recurrent Ovarian Germ Cell Tumor|Recurrent Primary Peritoneal Cavity Cancer etc./td
td style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229);MayoClinic/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);NCT01632332/td
td style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229);Recruiting/td
td style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229);HER2-positive Breast Cancer|Male Breast Cancer|Stage II Breast Cancer|Stage IIIA Breast Cancer|Stage IIIB Breast Cancer|Stage IIIC Breast Cancer/td
td style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229);MayoClinic|TapImmune,Inc./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);NCT01729884/td
td style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229);Recruiting/td
td style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229);HER2-positive Breast Cancer|Male Breast Cancer|Recurrent Breast Cancer|Stage IV Breast Cancer/td
td style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229);FredHutchinsonCancerResearchCenter|Fred Hutchinson Cancer Research Center/University of Washington Cancer Consortium|NationalCancerInstitute(NCI)/td
td style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229);2012-12/td
td style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229);Phase 2/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/ctep-s2861.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 CTEP (RO4956371) SDF/a/p
div class=clear-both style=margin: 0px; padding: 0px; clear: both; height: 0px; overflow: hidden; font-family: Arial, Tahoma, Helvetica; font-size: 12px; line-height: 19.200000762939453px;nbsp;/div
div class=clear style=margin: 0px; padding: 0px; zoom: 1; font-family: Arial, Tahoma, Helvetica; font-size: 12px; line-height: 19.200000762939453px;
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);391.77/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);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;19/spanHspan style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: 0.25em;13/spanClFspan style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: 0.25em;3/spanNspan style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: 0.25em;3/spanO/p
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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);871362-31-1/td
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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
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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
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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);nbsp;/td
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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);78 mg/mL (199 mM)/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);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
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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);10 mg/mL (25 mM)/td
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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);6 mg/mL/td
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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 style=margin: 0px; padding: 0px; font-family: Arial, Tahoma, Helvetica; font-size: 12px; line-height: 19.200000762939453px; height: 10px;nbsp;/div
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=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);Pyridine, 2-chloro-4-[2-[2,5-dimethyl-1-[4-(trifluoromethoxy)phenyl]-1H-imidazol-4-yl]ethynyl]-/td
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div class=clear-both style=margin: 0px; padding: 0px; clear: both; height: 0px; overflow: hidden; font-family: Arial, Tahoma, Helvetica; font-size: 12px; line-height: 19.200000762939453px;nbsp;/div
h3 id=chemicalInformation style=margin: 25px 0px 0px; padding: 0px; height: 25px; font-size: 14px; font-family: Arial, Tahoma, Helvetica; line-height: 19.200000762939453px;Preparing Stock Solutions/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=153px style=margin: 0px; padding: 5px 0px 5px 15px; font-weight: normal; border-style: solid; border-color: rgb(229, 229, 229);Stock Solution (1ml DMSO)/th
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);1mM/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);10mM/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);20mM/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);30mM/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);Mass(mg)/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);0.39177/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);3.9177/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);7.8354/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);11.7531/td
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