VU 0357121

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h1 itemprop=name style=margin: 0px 20px 0px 0px; padding: 0px; font-size: 24px; float: left;VU 0357121/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.S2795/span/div
p class=new_title style=margin: 5px 0px 10px; padding: 0px; clear: both; font-size: 11px; line-height: 14.399999618530273px;VU0357121 is a novel positive allosteric modulator (PAM) ofnbsp;b style=margin: 0px; padding: 0px;mGlu5/bnbsp;withnbsp;b style=margin: 0px; padding: 0px;EC50/bnbsp;of 33 nM, is inactive or very weakly antagonizing at other mGlu receptor subtypes./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 176/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 138/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 592/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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td colspan=6 style=margin: 0px; padding: 5px 15px; text-align: justify; border-style: solid; border-color: rgb(229, 229, 229);VU0357121 is a novel positive allosteric modulator (PAM) ofnbsp;b style=margin: 0px; padding: 0px;mGlu5/bnbsp;withnbsp;b style=margin: 0px; padding: 0px;EC50/bnbsp;of 33 nM, is inactive or very weakly antagonizing at other mGlu receptor subtypes./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
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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);33 nMnbsp;span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;a href=http://www.selleckchem.com/products/vu-0357121.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);VU0357121 do not bind at the MPEP allosteric site of mGlu5, thus do not possess mGlu5 NAM activity. The A809V/rmGlu5 mutation inhibited the ability of VU0357121 to shift the glutamate concentrationminus;response curve, whereas the response to VU0357121 is not altered by the F585I/rmGlu5 mutation.nbsp;span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;a href=http://www.selleckchem.com/products/vu-0357121.html#s_ref class=sref style=margin: 0px; padding: 0px; text-decoration: none; color: rgb(52, 84, 140); cursor: pointer;[1]/a/spannbsp;VU0357121 show weaker cooperativity in the Caspan style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;2+/spannbsp;mobilization assay in the low-expressing HEK293A-mGlu5 cell line.nbsp;span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;a href=http://www.selleckchem.com/products/vu-0357121.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);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);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);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/vu-0357121.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 Assay/th
td style=margin: 0px; padding: 5px 15px; text-align: justify; border-style: solid; border-color: rgb(229, 229, 229);The allosteric antagonist MPEP analogue [span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;3/spanH]methoxyPEPy is used to evaluate the ability of test compounds to interact with the MPEP site on mGlu5. Membranes are prepared from rat mGlu5 HEK293 cells. VU0357121 is diluted in assay buffer (50 mM Tris/0.9% NaCl, pH 7.4) to a 5times; stock, and 100 mu;L of the test compound is added to each well of a 96 deep-well assay plate. Three hundred microliter aliquots of membranes diluted in assay buffer (20 mu;g/well) are added to each well. One hundred microliters of [span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;3/spanH]methoxyPEPy (2 nM final concentration) is added, and the reaction is incubated at room temperature for 1 h with shaking. After the incubation period, the membrane-bound ligand is separated from free ligand by filtration through glass-fiber 96-well filter plates. The contents of each well are transferred simultaneously to the filter plate and washed 3minus;4 times with assay buffer using a cell harvester. Forty microliters of scintillation fluid is added to each well and the membrane-bound radioactivity determine by scintillation counting. Nonspecific binding is estimated using 5 mu;M MPEP. Concentrationminus;response curves are generated using a four parameter logistical equation in GraphPad Prism./td
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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=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/vu-0357121-s2795.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 VU 0357121 SDF/a/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);Molecular Weight (MW)/th
td width=55% style=margin: 0px; padding: 5px 0px 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);305.32/td
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p style=margin: 0px; padding: 0px;Cspan style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: 0.25em;17/spanHspan style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: 0.25em;17/spanFspan style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: 0.25em;2/spanNOspan style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: 0.25em;2/span/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);433967-28-3/td
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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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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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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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th width=12% rowspan=3 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);61 mg/mL (199 mM)/td
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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
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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);21 mg/mL (68 mM)/td
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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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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);4-butoxy-N-(2,4-difluorophenyl)benzamide/td
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/tbody
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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
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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);0.30532/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);3.0532/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);6.1064/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);9.1596/td
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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
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