• GW501516isapotentandselectiveperoxisomeproliferator-activatedreceptor(PPAR)β/δmodulator.
• Invitro,GW501516increasedexpressionofthereversecholesteroltransporterATP-bindingcassetteA1andinducedapolipoproteinA1-specificcholesterolefflux.Invivo,GW501516dramaticallyincreasedserumhighdensitylipoproteincholesterolwhileloweringthelevelsofsmall-denselowdensitylipoprotein,fastingtriglycerides,andfastinginsulinwhendosedtoinsulin-resistantmiddle-agedobeserhesusmonkeys.Oliver,W.R.Jr.,etal."Aselectiveperoxisomeproliferator-activatedreceptorδagoNISTpromotesreversecholesteroltransport."Proc.Natl.Acad.Sci.USA98:5306-5311(2001).
• TreatmentofskeletalmusclecellsbyGW501516resultedintheexpressionofgenesinvolvedinlipidutilization,β-oxidation,cholesterolefflux,andenergyuncoupling.FurThermore,thetreatmentalsoincreasedapolipoprotein-A1specificeffluxofintracellularcholesterol,indicatingthemuscletissueisanimportanttargetofPPARβ/δagonists.Dressel,U.,etal."Theperoxisomeproliferator-activatedreceptorβ/δagonist,GW501516,regulatestheexpressionofgenesinvolvedinlipidcatabolismandenergyuncouplinginskeletalmusclecells."Mol.Endocrinol.17:2477-2493(2003).
• GW501516inducedfattyacidβ-oxidationinL6myotubesandinmouseskeletalmuscles.GW501516treatmenttomicefedahigh-fatdietameliorateddiet-inducedobesityaswellasinsulinresistance.GW501516treatmentalsodramaticallyimproveddiabetes,asdemonstratedbythedecreaseinplasmaglucoseandbloodinsulinlevelsingeneticallyobeseob/obmice.Tanaka,T.,etal."Activationofperoxisomeproliferator-activatedreceptorδinducesfattyacidβ-oxidationinskeletalmuscleandattenuatesmetabolicsyndrome."Proc.Natl.Acad.Sci.USA100:15924-15929(2003).
• GW501516protectedagainstcytotoxin-inducedSH-SY5Ycellinjuryinvitro.ItalsosignificantlyattenuatedtheischemicbraindamageandMPTP-induceddepletionofstriataldopamineandrelatedmetabolitecontentsinmousebrain.Iwashita,A.,etal."Neuroprotectiveefficacyoftheperoxisomeproliferator-activatedreceptorδ-selectiveagonistsinvitroandinvivo."J.Pharmacol.Exp.Ther.320:1087-1096(2007).
• GW501516treatmentdidnotstimulatethegrowthofhumancancercelllinesincludingHT29,HCT116,LS-174T,HepG2,andHuH7.Hollingshead,H.E.,etal."Peroxisomeproliferator-activatedreceptor-β/δ(PPARβ/δ)ligandsdonotpotentiategrowthofhumancancercelllines."Carcinogenesis28:2641-2649(2007).
• GW501516wasidentifiedasanorallyactiveagentthatwouldmimicorpotentiatetheeffectsofexercise.Narkar,V.A.,etal."AMPKandPPARδagonistsareexercisemimetics."Cell134:405-415(2008).
• GW501516reducedtheIFNγ-inducedup-regulationofTNFαandinducIBLeNOsynthase,andshowedanti-inflammatoryactivity.Defaux,A.,etal."EffectsofthePPAR-βagonistGW501516inaninvitromodelofbraininflammationandantibody-induceddemyelination."J.Neuroinflammation6:15(2009).
• AnotherCASnumberpreviouslyassignedtoGW501516freeacid,namely813458-54-7,hasbeendeletedbyCASandisnolongerinuse.
• STRUCTUREERRORONWIKIPEDIA"SGW501516PAGE:AsofDecember21,2012,thestructureshownontheWikipediapageforGW501516isnotcorrect--theversionshownonWikipediaismissingamethylgrouponthebenzeneringcarryingsulfur-andoxygen-bearingsubstituents.
• Soldforlaboratoryormanufacturingpurposesonly;notforhuman,veterinary,food,orhouseholduse.
• ThisproductisofferedforR&Duseinaccordancewith(i)35USC271(e)+A13(1)intheU.S.;(ii)Section69.1ofJapanesePatentLawinJapan;(iii)Section11,No.2oftheGermanPatentActof1981inGermany;(iv)Section60,Paragraph5boftheU.K.PatentsActof1977intheU.K.;(v)Sections55.2(1)and55.2(6)andothercommonlawexemptionsofCanADIanpatentlaw;(vi)Section68BofthePatentsActof1953inNewZealandtogetherwiththeamendmentofsamebytheStatutesAmendmentBillof2002;(vii)suchrelatedlegislationand/orcaselawasmaybeorbecomeapplicableintheaforementionedcountries;and(viii)suchsimilarlawsandrulesasmayapplyinvariousothercountries.
• Notavailableinsomecountries;notavailabletosomeinstitutions;notavailableforsomeuses.

Storage

Solubility

Disposal