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PotentandselectiveFFA4(GPR120)agonist(pEC50valuesare6.3,6.2and6.1atthehuman,mouseandratreceptor,respectively).Exhibits≥100-foldselectivityagainstapanelof61targetsincludingFFA1,FFA2andFFA3.Enhancesglucose-stimulatedinsulinsecretioninMIN6cells.InducesintracellularcalciumaccumulationinU2OScells;thisactivityisinhibitedbyAH7614(Cat.No.5256).
SoldforresearchpurposesunderagreementfromGlaxoSmithKline
GSK137647isalsoofferedaspartoftheTocriscreenPlus.FindoutmoreaboutcompoundlibrariesavailablefromTocris.
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
Thefollowingdataisbasedontheproductmolecularweight305.39.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
Referencesarepublicationsthatsupporttheproducts'biologicalactivity.
Sparksetal(2014)Identificationofdiarylsulfonamidesasagonistsofthefreefattyacidreceptor4(FFA4/GPR120).Bioorg.Med.Chem.Lett.243100PMID:24881566
Martinetal(2012)Lipid-mediatedreleaseofGLP-1bymousetastebudsfromcircumvallatepapillae:putativeinvolvementofGPR120andimpactontastesensitivity.J.LipidRes.532256PMID:22904345
Keywords:GSK137647,supplier,GSK137647,Free,fatty,acid,receptor,4,diabetes,potent,and,selective,FFA4,GPR120,agonist,Free,Fatty,Acid,Receptors,Free,Fatty,Acid,Receptors,TocrisBioscience
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