ZG-2686-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEZG-2686Cat.No.:HY-179647CASNo.:1795110-22-3分⼦式:C₁₃H₉BrN₄O分⼦量:317.14作⽤靶点:HIF/HIFProlyl-Hydroxylase作⽤通路:MetabolicEnzyme/Protease储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性ZG-2686⼀种强效的选择性HIF-2α激动剂，EC50为0.25µM。ZG-2686对PHD2具有选择性。ZG-2686与HIF-2α的特定内部空腔结合，通过结构⽔分⼦形成氢键，从⽽稳定HIF-2α/β异⼆聚体并增强其转录活性。ZG-2686与Vadadustat(HY-101277)具有协同作⽤，可在体外和体内上调HIF-2α依赖的EPO因表达。ZG-2686可⽤于肾性贫⾎的研究[1]。IC50&TargetHIF-2α0.25μM(EC50)体外研究ZG-2686demonstratesgoodinvitrometabolicstabilityinratplasmaandlivermicrosomes[1].ZG-2686(10-20μM;12h)showsasynergisticupregulationofHIF-2α-dependentEPOmRNAlevelinHep3BcellswhencombinedwithVadadustat[1].RealTimeqPCR[1]CellLine:Hep3BcellsConcentration:10,20μMIncubationTime:12hResult:HadminimaleffectonEPOmRNAlevel.ProducedasynergisticeffectwhencombinedwithVadadustat.IncreasedEPOgeneexpressionby4.35-foldat20μMwhencombinedwithVadadustat(20μM).1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE体内研究ZG-2686(10and20mg/kg;i.p.;singledose)showslimitedinvivoEPOinductionalonebutsynergizeswithVadadustattoenhanceEPOexpressioninC57BL/6mice[1].AnimalModel:MaleC57BL/6mice(6-8weeksold,18-22g)[1]Dosage:10and20mg/kgAdministration:i.p.;singledoseResult:HadminimaleffectonEPOmRNAlevel.SynergisticallyincreasedEPOgeneexpressionwhencombinedwiththePHDinhibitorVadadustat.REFERENCES[1].GaoY,etal.Discoveryof3-(Arylamido)pyrazolopyridineHIF-2αAgonistsandaCodrugStrategywithProlylHydroxylaseInhibitionforSynergisticTreatmentofRenalAnemia.JMedChem.2025;68(23):25569-25589.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-820-37