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TAK-875isanorally-available,benzofuran-based,agoNISTofGPR40forthepotentialtreamentofType2diabetesmellitus,withanhumanEC50of0.014uMinaFLIPRassay.IthashighselectivityoverGPR41,GPR43,andGPR120,withEC50sallgreaterthan10uM.[1]Oraldosing(0.3-3mg/kg)ofTAK-875inaglucoseintolerancetestinfemaleWistarratsreducedbloodglucoseexcursion.Insulinsecretionwasincreasedduringanoralglucosetolerancetest.
TAK-875wasshowntoactivatetheGqa-mediatedsignallingpathwayinpancreaticb-cells.ProlongedagoniststimulationbyTAK-875revealednoevidenceofb-celldysfunctionortoxicity,nordoesitcauseainductionofaMarkerofapoptosisinpancreaticb-cells.[2]
Technicalinformation:
| ChemicalFormula: | C29H32O7S.1/2H2O | |
| CAS#: | 1000413-72-8 | |
| MolecularWeight: | 533.63 | |
| Purity: | >98% | |
| Appearance: | White | |
| ChemicalName: | [(3S)-6-({2,6-dimethyl-4-[3-(methylsulfonyl)propoxy]biphe-nyl-3-yl}meth-oxy)-2,3-dihydro-1-benzofuran-3-yl]aceticacidhemi-hydrate | |
| Solubility: | Upto100mMinDMSO | |
| Synonyms: | TAK-875,TAK875 |
ShippingCondition:Theproductisshippedinaglassvialatambienttemperature.
Storagecondition:Forlongershelflife,storesolidpowderat4oCdesiccated,orstoreDMSOsolutionat-20oC.
Reference:
| 1. | Negoroetal.,ACSMed.Chem.Lett.2010,1,290-294. |
| 2. | Tsujihataetal.,TAK-875,anorallyavailableGprotein-coupledreceptor40/freefattyacidreceptor1agonist,enhancesglucose-dependentinsulinsecretionandimprovesbothpostprandialandfastinghyperglycemiaintype2diabeticrats.J.Pharmacol.Exp.Ther.2011,339(1),228-237.PubmedID:21752941 |