Saralasin-Sar1-Ala8-Angiotensin-II-DataSheet-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemESaralasinCat.No.:HY-P0205CASNo.:34273-10-4Synonyms:[Sar1,Ala8]AngiotensinII分⼦式:C₄₂H₆₅N₁₃O₁₀分⼦量:912.05Sequence:{Sar}-Arg-Val-Tyr-Val-His-Pro-AlaSequenceShortening:{Sar}-RVYVHPA作⽤靶点:AngiotensinReceptor作⽤通路:GPCR/GProtein储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性Saralasin([Sar1,Ala8]AngiotensinII)⾎管紧张素II(angiotensinII)的⼋肽类似物。Saralasin⼀种竞争性的⾎管紧张素II受体(angiotensinIIreceptor)拮抗剂，Ki值为0.32nM(74%的结合位点)，并具有部分激动剂活性。Saralasin可⽤于肾⾎管性⾼⾎压、肾素依赖性（⾎管紧张素原性）⾼⾎压的相关研究[1][3][6]。IC50&TargetKi:0.32nM(AngiotensinIIreceptor)[3]体外研究Saralasin(1nM,48or72h)inhibitscellgrowthin3T3andSV3T3cells[1].Saralasin(5μM,2h)restoresIto,fast(Fast-InactivatingTransientOutwardK+CurrentinMouseVentricle)andIK,slow(Slow-InactivatingTransientOutwardK+CurrentinMouseVentricl)tocontrollevelsinmyocytes[2].Saralasin(0.1-10nM,40min)inhibitsbindingofFITC-AngIItoratlivermembranepreparation(usedasthesourceofangiotensinreceptors)withaKivalueof0.32nMfor74%ofthebindingsitesand2.7nMfortheremainingbindingsites[3].Saralasin(1μM,perfusedratovaryinvitro)inhibitstheovulationrateversuscontrolandreducesprostaglandinE2and6-keto-prostaglandinF1αlevels[4].CellProliferationAssay[1]CellLine:3T3andSV3T3cells1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEConcentration:1nMIncubationTime:48h,72hResult:Inhibitedcellgrowthin3T3andSV3T3cellsandcausedanincreaseofcellularreninconcentration.体内研究Saralasin(intravenousinjection,5-50μg/kg,asingledose)amelioratestheoxidativestressandtissueinjuryincerulein-inducedpancreatitis[5].Saralasin(subcutaneousinjection,10and30mg/kg,asingledose)increasesserumreninactivity(SRA)innormal,consciousrats,withoutmarkedlyalteringbloodpressureorheartrate[6].AnimalModel:Cerulein-inducedacutepancreatitisratsmodel[5]Dosage:5,10,20,and50μg/kg,asingledose.Administration:IntravenousinjectionResult:Restoredthepancreaticmorphologicalcharacteristicstothecontrollevel.Reducedpancreaticinjuryandsuppressedtheglutathionedepletioninducedbycerulean.AnimalModel:MaleSprague-Dawleyrats[6]Dosage:10and30mg/kg,asingledose.Administration:SubcutaneousinjectionResult:Stimulatedreninreleasewithoutalteringbloodpressureorheartrateatthetimeofmeasuringserumreninlevels20minutesafterinjection.REFERENCES[1].PSchelling,etal.EffectsofangiotensinIIandangiotensinIIantagonistsaralasinoncellgrowthandreninin3T3andSV3T3cells.JCellPhysiol.1979Mar;98(3):503-13.[2].JeremyHKim,etal.Pressure-overload-inducedangiotensin-mediatedearlyremodelinginmouseheart.PLoSOne.2017May2;12(5):e0176713.[3].MaziarMohammadAkhavan,etal.Anon-radioactivemethodforangiotensinIIreceptorbindingstudiesusingtheratliver.JPharmacolToxicolMethods.2006May-Jun;53(3):206-14.[4].MMikuni,etal.Saralasin-inducedinhibitionofovulationintheinvitroperfusedratovaryisnotreplicatedbytheangiotensinIItype-2receptorantagonistPD123319.AmJObstetGynecol.1998Jul;179(1):35-40.[5].SiuPoIp,etal.Saralasin,anonspecificangiotensinIIreceptorantagonist,attenuatesoxidativestressandtissueinjuryincerulein-inducedacutepancreatitis.Pancreas.2003Apr;26(3):224-9.[6].CampbellWB,etal.Saralasin-inducedreninrelease:itsblockadebyprostaglandinsynthesisinhibitorsintheconsciousrat.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEHypertension.1979;1(6):637‐642.McePdfHeightCaution:Pr