GW501516isaselectivePPARdagonistwithaKiaffinityof1.1nMinahumanbindingassay.Inacell-basedtransfectionassay,GW501516inducesexpressionofGAL4-responsivereportergeneatanEC50of1.2nM.Atdosesupto1uM,GW501516doesnotpromoteadipocytedifferentiation,bindtoRXRa,orhaveactivitytowardothernuclearornon-nuclearreceptors.(1)GW501516incrasesexpressionofthereversecholesteroltransporterATP-bindingcassetteA1andinducesapolipoproteinA1-specificcholesterolefflux.(1)
GW501516isalsoreportedtobeaPPARbagonistwithanti-inflammatoryactivityanddecreasesIFN-g-inducedupregulationofTNF-aandiNOS.Concurrently,GW501516increaseIL-6mRNAexpression.(2)
Technicalinformation:
| ChemicalFormula: | C21H18F3NO3S2 | |
| CAS#: | 317318-70-0 | |
| MolecularWeight: | 453.5 | |
| Purity: | >98% | |
| Appearance: | white | |
| ChemicalName: | 2-(2-methyl-4-((4-methyl-2-(4-(trifluoromethyl)phenyl)thiazol-5-yl)methylthio)phenoxy)aceticacid | |
| Solubility: | Upto22mMinDMSO | |
| Synonyms: | GW501516,GW-501,516,GW1516,GSK-516,Endurobol |
ShippingCondition:Theproductisshippedinaglassvialatambienttemperature.
Storagecondition:Forlongershelflife,storesolidpowderat4oCdesiccated,orstoreDMSOsolutionat-20oC.
Reference:
| 1. | Oliveretal.,Aselectiveperoxisomeproliferator-activatedreceptordagonistpromotesreversecholesteroltransport.Proc.Natl.Acad.Sci.2001,98(9),5306-5311.PubmedID:11309497 |
| 2. | Defauxetal.,EffectsofthePPAR-bagonistGW501516inaninvitromodelofbraininflammationandantibody-induceddemyelination.J.Neuroinflammation,2009,6,15-27.PubmedID:19422681 |