GPR81-agonist-1-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•Agonists•ScreeningLibrariesGPR81agonist1Cat.No.:HY-135982CASNo.:1620992-67-7分⼦式:C₂₂H₃₀N₄O₂S₂分⼦量:446.63作⽤靶点:Others作⽤通路:Others储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性GPR81agonist1⼀种⾼效、⾼选择性的GPR81激动剂，对⼈和⼩⿏GPR81的EC50分别为58nM和50nM。GPR81agonist1抑制分化的3T3-L1脂细胞的脂解。GPR81agonist1抑制⼩⿏的脂解并不会造成⽪肤潮红。GPR81agonist1对GPR81的选择性⾼于GPR109a。体外研究GPR81agonist1(compound2)(1-1000nM)inhibitslipolysisindifferentiated3T3-L1adipocytes[1].体内研究GPR81agonist1(100mg/kg;i.p.)suppresseslipolysisinmicewithoutcutaneousflushing[1].GPR81agonist1(10mg/kg;i.p.)showsgoodbioavailability(71%)andCmax(6.3μM)[1].AnimalModel:Nine-week-oldmaleC57/Bl6mice(fedandfastedmice)[1]Dosage:100mg/kgAdministration:I.p.Result:ReducedplasmaFFAcontentoffedandfastedmicebyapproximately50%and35%,respectively,at15minpostdosewhenintraperitoneallyadministeredatadoseof100mg/kg.AnimalModel:MaleC57/Bl6mice[1]Dosage:10mg/kg(PharmacokineticAnalysis)Administration:I.p.(PharmacokineticAnalysis)1/2Result:Showedgoodbioavailability(71%)andCmax(6.3μM).REFERENCES[1].SakuraiT,etal.IdentificationofanovelGPR81-selectiveagonistthatsuppresseslipolysisinmicewithoutcutaneousflushing.EurJPharmacol.2014;727:1-7.McePdfHeightMedChemExpress(MCE)只为有资质的科研机构、医药企业基于科学研究或药证申报的⽤途提供医药研发服务，不为任何个⼈或者⾮科研性质的、⾮⽤于药