Aliskiren-hydrochloride-CGP-60536-hydrochloride-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEAliskirenhydrochlorideCat.No.:HY-12176ACASNo.:173399-03-6Synonyms:CGP60536hydrochloride;CGP60536Bhydrochloride;SPP100hydrochloride分⼦式:C₃₀H₅₄ClN₃O₆分⼦量:588.22作⽤靶点:Renin;Autophagy作⽤通路:MetabolicEnzyme/Protease;Autophagy储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性Aliskiren(CGP60536;CGP60536B;SPP100)hydrochloride⼀种⼝服有效的、选择性的肾素(renin)抑制剂，IC50为1.5nM。Aliskirenhydrochloride可⽤于⾼⾎压、⼼⾎管疾病和癌症恶病质的研究。IC50&TargetIC50:1.5nM(renin)[1];0.6nM(humanrenin),2nM(marmosetrenin),80nM(ratrenin),7nM(dogrenin),11nM(rabbitrenin),63nM(guineapigrenin),150nM(pigrenin)[2]体外研究Aliskirenhydrochlorideinhibitsplasmareninactivity(PRA)invitrowithIC50sof2.9nM(humanPRA),8.0nM(monkeyPRA),respectively[1].Aliskirenhydrochloride(10μM;24h)inhibitsprorenin-inducedhumanaorticsmoothmusclecellmigration[2].Aliskirenhydrochloride(1-10μM;24h)inhibitsboththelamellipodiaformationandmorphologicalchangesinducedbyproreninwithnosignificanteffectonPDGF-BBactivity[2].CellMigrationAssay[2]CellLine:Smoothmusclecell(SMC)Concentration:1-10μMIncubationTime:24hoursResult:Inhibitedhumanaorticsmoothmusclecellmigrationinducedbyprorenin(10nM)at10μ1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEM.体内研究Aliskirenhydrochloride(3mg/kg,10mg/kg;p.o.;daily;0-12d)inhibitreninandlowerbloodpressurewithoutaffectingheartrateinsodium-depletedmarmosets[3].Aliskirenhydrochloride(10mg/kg;p.o.;singledose)delayscachexiadevelopment,reducestumor,andprolongsmousesurvival.Andalsoimproveswhole‑bodystrength,mobilityandcoordination,enhanceslocomotoractivity,andinhibitsmusclewasting[4].Aliskirenhydrochloride(10mg/kg;p.o.;singledose;20dafterC26injection)reducesoxidativestressassociatedwithcancercachexia[4].AnimalModel:Sodium-depletedmarmosets[3]Dosage:3mg/kg,10mg/kgAdministration:Oralgavage;oncedaily;12daysResult:Increasedplasmaimmunoreactivereninlevels,andloweredbloodpressurewithoutaffectingheartrate.ShowednoreboundincreaseinBPfollowingtheendoftreatmentwitheitherdoseofaliskiren.InhibitedtheRASandcontrolstheupregulationofpro‑inflammatorycytokines.AnimalModel:CancercachexiamodelinBALB/cmiceinjectedwithC26mousecoloncarcinomacells[4]Dosage:10mg/kgAdministration:Oralgavage;onday5(asapreventivestrategy,APgroup)oronday12(asatherapeuticstrategy,ATgroup)afterC26injection;for20daysafterC26injectionResult:Enhancedgripstrength,coordination,andlocomotoractivity.InhibitedserumAngIandⅡlevelsandbothserumandmusculartumornecrosisfactor

‑α(TNF‑α)andinter‑leukin‑6(IL‑6)levels.户使⽤本产品发表的科研⽂献•NeurobiolDis.2014Nov;71:292-304.•LipidsHealthDis.2018Jul31;17(1):183.•ToxicologyResearchandApplication.2018,2:239784731880115.•ToxicologyResearchandApplication.September25,2018.•DepartmentofBiologicalScience.NationalSunYat-SenUniversity.2015Sep.Seemorecustomervalidationsonwww.MedChemE2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEREFERENCES[1].YujiNakamura,etal.DiscoveryofDS-8108b,aNovelOrallyBioavailableReninInhibitor.ACSMed.Chem.Lett.,2012,3(9),pp754–758[2].WoodJM,etal.Structure-baseddesignofaliskiren,anovelorallyeffectiverenininhibitor.BiochemBiophysResCommun.2003Sep5;308(4):698-705.[3].WangC,etal.Aliskirentargetsmultiplesystemstoalleviatecancercachexia.OncolRep.2016Nov;36(5):3014-3022.[4].FerriN,etal.Aliskireninhibitsprorenin-inducedhumanaorticsmoothmusclecellmigration.JReninAngiotensinAldosteroneSyst.2015Jun;16(2):284-91.McePdfHeightCaut