INCB13739-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEINCB13739Cat.No.:HY-150701CASNo.:869974-19-6分⼦式:C₂₈H₂₅N₃O₄分⼦量:467.52作⽤靶点:GlucocorticoidReceptor;MineralocorticoidReceptor作⽤通路:Immunology/Inflammation;MetabolicEnzyme/Protease储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性INCB13739⼀种⼝服有效的、选择性的和组织特异性11β-HSD1(11β-羟类醇脱氢酶1)抑制剂，IC50值分别为3.2nM(11β-HSD1酶)和1.1nM(11β-HSD1PBMC)。INCB13739可⽤于2型糖尿病(T2DM)和肥胖研究。IC50&TargetIC50:3.2nM(11β-HSD1enzymatic),1.1nM(11β-HSD1PBMC)[1]体外研究INCB13739is>1000-foldselectivetowards11β-HSD2,mineralocorticoidreceptor(MR),andglucocorticoidreceptor(GR)[1].体内研究INCB13739(Orally)iseffectivelydistributedintheadiposetissueandisinhibiting11β-HSD1activity>90%foratleast24hpost-dose[1].INCB13739(3mg/kg,IV;10mg/kg,PO;once)displaysdecentoralbioavailabilityinbothratsandcynomolgusmonkeys[1].PharmacokineticParametersofINCB13739inrats[1].IV(3mg/kg)PO(10mg/kg)Cmax(µM)6.46±2.41AUC0-24(ng/mL∗h)11.2±3.27t1/2(h)1.4±0.21.2±0.3CL((L/h)/kg)1.0±0.2Vdss(L/kg)1.6±0.5F(%)51±15AnimalModel:Rats,cynomolgusmonkeys[1]Dosage:3mg/kg(IV),10mg/kg(PO)Administration:IVandPO,once(PharmacokineticAnalysis)1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEResult:Displayeddecentoralbioavailabilityinbothrats(F%=51±15%)andcynomolgusmonkeys(F%=43%).REFERENCES[1].MarandoC,etal.Discoveryof1'-(1-phenylcyclopropane-carbonyl)-3H-spiro[isobenzofuran-1,3'-pyrrolidin]-3-oneasanovelsteroidmimeticscaffoldforthepotentandtissue-specificinhibitionof11β-HSD1usingascaffold-hoppingapproach.BioorgMedChemLett.2022Aug1;69:128782.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-820-379