Perindoprilat-S-9780-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEPerindoprilatCat.No.:HY-B1433CASNo.:95153-31-4Synonyms:S9780分⼦式:C₁₇H₂₈N₂O₅分⼦量:340.41作⽤靶点:Angiotensin-convertingEnzyme(ACE)作⽤通路:MetabolicEnzyme/Protease储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性Perindoprilat(S9780)⼀种⾎管紧张素转化酶(ACE)抑制剂，IC50值为1.5-3.2nM，Perindoprilat可⽤于⾼⾎压的研究。体外研究Perindoprilat(1μM,10days)treatmentsuppressestheangiotensinIIproductioninHNSCCcells[2].Perindoprilat(40μM,3days)treatmentattenuatesmesangialcellfibronectinlevel[3].CellViabilityAssay[2]CellLine:HNSCCcellsConcentration:1μMIncubationTime:10daysResult:SuppressedtheangiotensinIIproductioninHNSCCcells(P=0.028).CellViabilityAssay[3]CellLine:HumanmesangialcellsConcentration:40μMIncubationTime:3days1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEResult:ResultedindecreasesinMPCM-stimulatedfibronectinlevelsof19.4±0.6%(P<0.001)and21.7±1.0%(P<0.001)forsecretedandcell-associatedfibronectinlevels,respectively.体内研究Perindoprilat(oralgavage;1.5mg/kg;oncedaily;7d)treatmentimprovescardiacfunctioninmicewithacutemyocardialinfarctionandreducesthenumberofapoptoticmyocardialcells[4].Perindoprilat(oralgavage;1.5mg/kg;oncedaily;7d)treatmentreducestheexpressionlevelsofmyocardialBaxandBcl-2ininfarctionzonesofmicewithacutemyocardialinfarction[4].Perindoprilat(oralgavage;1.5mg/kg;oncedaily;7d)treatmentlowerstheexpressionofmyocardialTLR4/NF-κBininfarctionzonesinmicewithacutemyocardialinfarction[4].AnimalModel:C57BL/6Jmiceunderwentcoronaryligation[4]Dosage:1.5mg/kgAdministration:Oralgavage;1.5mg/kg;oncedaily;7daysResult:Exhibitedmarkedlyloweredthenumberofapoptoticmyocardialcellsincomparisonwiththeacutemyocardialinfarctiongroup(p<0.05).AnimalModel:C57BL/6Jmiceunderwentcoronaryligation[4]Dosage:1.5mg/kgAdministration:Oralgavage;1.5mg/kg;oncedaily;7daysResult:ReducedthegeneandproteinexpressionlevelsofBax(amyocardialapoptosisgene)ininfarctionzonesinmicewithacutemyocardialinfarction.AnimalModel:C57BL/6Jmiceunderwentcoronaryligation[4]Dosage:1.5mg/kgAdministration:Oralgavage;1.5mg/kg;oncedaily;7daysResult:DeclinedthenumberofstainedNF-κBp50proteininthenucleusininfarctionzones(p<0.05),comparedtotheacutemyocardialinfarctiongroup.REFERENCES[1].Perindopril.ExpertOpinPharmacother.2006Jan;7(1):63-71.[2].Angiotensin-convertingenzyme(ACE)inhibitorshavedifferentselectivityforbradykininbindingsitesofhumansomaticACE.EurJPharmacol.2007Dec22;577(1-3):1-6.[3].IzabellaZAPawluczyk,etal.Theroleofbradykininintheantifibroticactionsofperindoprilatonhumanmesangialcells.KidneyInt.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE2004Apr;65(4):1240-51.McePdfHeightCaution:Producthasnotbeenfullyvalidatedfo