Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemERORγtInverseagonist10Cat.No.:HY-133552CASNo.:2413986-35-1分?式:C??H??F?N?O?分?量:572.5作?靶點:ROR作?通路:MetabolicEnzyme/Protease儲存?式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY?物活性RORγtInverseagonist10?種有效、有?服活性的RORγt反向激動劑，IC50值為51nM。RORγt銀屑病發病機制相關的IL-17A、IL-22、IL-23r等因的主轉錄因?[1]。IC50&TargetRORγt51nM(IC50)體外研究RORγtInverseagonist10hasagoodlivermicrosomestability(humanCLint=0.010mL/min/mg,mouseCLint=0.030mL/min/mg)[1].RORγtInverseagonist10suppressestheIL-17Aproductioninadose-dependentmannerwithanIC50of130nMinahumanwhole-bloodassay[1].體內研究RORγtInverseagonist10(3-100mg/kg;p.o.)showsrobustanddose-dependentinhibitoryeffectontheIL-17AproductioninmouseIL-18/23-inducedcytokineexpressionmodel[1].RORγtInverseagonist10(1.145mg/kg;p.o.)showsahighAUCof15000nM*handt1/2of3.6hours[1].AnimalModel:C57/BL6malemice,mouseIL-18/23-inducedcytokineexpressionmodel[1]Dosage:3mg/kg,10mg/kg,30mg/kg,100mg/kgAdministration:OraladministrationResult:SignificantlyinhibitedtheIL-17Aproductioninadose-dependentmanner.1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEAnimalModel:Mice[1]Dosage:1.145mg/kg(PharmacokineticAnalysis)Administration:OraladministrationResult:AUC=15000nM*h,t1/2=3.6hours.REFERENCES[1].RyotaNakajima,etal.Discoveryof[1,2,4]Triazolo[1,5-a]pyridineDerivativesasPotentandOrallyBioavailableRORγtInverseAgonists.ACSMedChemLett.2020Feb27;11(4):528-534.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-820-3792;021