Vardenafil-dihydrochloride-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEVardenafildihydrochlorideCat.No.:HY-B0442CCASNo.:224789-15-5分⼦式:C₂₃H₃₄Cl₂N₆O₄S分⼦量:561.52作⽤靶点:EndogenousMetabolite;Phosphodiesterase(PDE)作⽤通路:MetabolicEnzyme/Protease储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性Vardenafildihydrochloride⼀种具有⾼选择性和⼝服活性的磷酸⼆酯酶5(PDE5)抑制剂，IC50为0.7nM。Vardenafildihydrochloride对PDE1、PDE6的IC50分别为180nM和11nM，对PDE3、PDE4的IC50>1000nM。Vardenafildihydrochloride⾮竞争性地抑制环磷酸鸟苷(cGMP)⽔解，从⽽提⾼cGMP⽔平。Vardenafildihydrochloride可⽤于研究勃起功能障碍、肝炎、糖尿病等。IC50&TargetPDE5PDE1PDE60.7nM(IC50)180nM(IC50)11nM(IC50)体外研究VardenafildihydrochloridespecificallyinhibitsthehydrolysisofcGMPbyPDE5withanIC50valueof0.7nM[1].VardenafildihydrochlorideincreasesintracellularcGMPlevelsinthecavernosumtissueofthepenis,thusresultsincreasingthedilationofthebody'ssinusesandbloodflow[3].体内研究Vardenafildihydrochloride(0.03mg/kg;i.v.)exhibitsfacilitatoreffectsinratswithcavernousnerveinjury[4].Vardenafildihydrochloride(0.17mg/kg;i.v.;oncedaily;7d)protectsliveragainstConA–inducedhepatitis,anddecreasestheexpressionofNF-휅BandiNOSinhepatictissue[5].Vardenafildihydrochloride(10mg/kg;p.o.;oncedaily;25weeks)preventsthereductionoftissuecGMPlevelsandtheincreasein3-NTgenerationinZDFhearts[6].AnimalModel:Malerat(9-week-old)underwentsurgeryforlaparotomyorbilateralcavernousnerve(CN)crushinjury[4]Dosage:0.03mg/kg1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEAdministration:IntravenousinjectionResult:RestorednormalerectileresponseswithacombindadministrationofBAY60-4552(0.03,0.3mg/kg).AnimalModel:LiverinjuryinducedbyConAinmaleSwissalbinomice(20±2g)[5]Dosage:0.17mg/kgAdministration:Intravenousinjection;oncedaily,for7days;asapretreatmentResult:ReducedthelevelsofserumtransaminasesandalleviatedConA-inducedhepatitis.AnimalModel:Male7-week-oldZuckerdiabeticfatty(ZDF)rats(preservedejectionfraction,HFpEF)[6]Dosage:10mg/kgAdministration:Oralgavage;oncedaily,for25weeksResult:Improvedmyofilamentfunctionindiabeticrathearts.户使⽤本产品发表的科研⽂献•AnimCellsSyst(Seoul).2019May16;23(3):155-163.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].AshourAE,etal.Vardenafildihydrochloride.ProfilesDrugSubstExcipRelatMethodol.2014;39:515-544.[2].SaenzdeTejadaI,etal.ThephosphodiesteraseinhibitoryselectivityandtheinvitroandinvivopotencyofthenewPDE5inhibitorvardenafil.IntJImpotRes.2001;13(5):282-290.[3].GresserU,etal.Erectiledysfunction:comparisonofefficacyandsideeffectsofthePDE-5inhibitorssildenafil,vardenafilandtadalafil--reviewoftheliterature.EurJMedRes.2002Oct29.7(10):435-46.[4].OudotA,etal.CombinationofBAY60-4552andvardenafilexertsproerectilefacilitatoreffectsinratswithcavernousnerveinjury:aproofofconceptstudyforthetreatmentofphosphodiesterasetype5inhibitorfailure.EurUrol.2011Nov.60(5):1020-6.[5].AhmedN,etal.Hepatoprotectiveroleofvardenafilagainstexperimentallyinducedhepatitisinmice.JBiochemMolToxicol.2017Mar.31(3).[6].BódiB,etal.Long-TermPDE-5AInhibitionImprovesMyofilamentFunctioninLeftandRightVentricularCardiomyocytesthroughPartiallyDifferentMechanismsinDiabeticRatHearts.Antioxidants(Basel).2021Nov6.10(11):1776.McePdfHeightCaution:Productha