Fonsartan-HR-720-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEFonsartanCat.No.:HY-19224CASNo.:153235-15-5Synonyms:HR720分⼦式:C₂₆H₃₀K₂N₄O₅S₂分⼦量:620.87作⽤靶点:AngiotensinReceptor作⽤通路:GPCR/GProtein储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性Fonsartan(HR720)⼀种AT1受体拮抗剂。Fonsartan可⽤于⼼肌梗死(MI)的研究[1][2]。IC50&TargetAT1Receptor体外研究FonsartanselectivelyinhibitsAT1receptors(mainlyintheadrenalcortex(IC50=1.5×10-8M))whilehavingaloweraffinityforAT2receptors(mainlyintheadrenalmedulla(IC50=1.4×10-6M))[2].体内研究Fonsartan(3mg/kg,s.c.,oncedailyfor6weeks)producesthemostcomprehensivecardioprotectiveeffectwhenadministeredtoratswithmyocardialinfarction(MI)modelingstarting3to24hoursaftermodeling[1].AnimalModel:Amyocardialinfarction(MI)modelwasinducedinmalenormotensiveWistarrats(weighing250-280g)byligatingtheleftanteriordescendingcoronaryartery[1].Dosage:3mg/kgAdministration:S.c.,oncedailyfor6weeksResult:Administrationat30min,3h,24h,and7dpost-administrationallinhibitedmyocardialhypertrophy.Administrationat3hand24hpost-administrationsignificantlyreducedinfarctsize.Limitedeffectonimprovingleftventriculardilation(LVD,LVC).REFERENCES1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE[1].XiaQG,etal.SignificanceoftimingofangiotensinAT1receptorblockadeinratswithmyocardialinfarction-inducedheartfailure.CardiovascRes.2001Jan;49(1):110-7.[2].JinD,etal.Pharmacologicalprofilesofanovelnon-peptideangiotensinIItypeIreceptorantagonistHR720invitroandinvivo.JpnJPharmacol.1997Nov;75(3):259-66.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-820-3792