Y-27632-dihydrochloride-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEY-27632dihydrochlorideCat.No.:HY-10583CASNo.:129830-38-2分⼦式:C₁₄H₂₃Cl₂N₃O分⼦量:320.26作⽤靶点:ROCK作⽤通路:CellCycle/DNADamage;Cytoskeleton;StemCell/Wnt;TGF-beta/Smad储存⽅式:4°C,sealedstorage,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoisture)溶解性数据体外实验H2O:100mg/mL(312.25mM;Needultrasonic)DMSO:33.33mg/mL(104.07mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM3.1225mL15.6123mL31.2246mL5mM0.6245mL3.1225mL6.2449mL10mM0.3122mL1.5612mL3.1225mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month(sealedstorage,awayfrommoisture)。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。体内实验请根据您的实验动物和给药⽅式选择适当的溶解⽅案。以下溶解⽅案都请先按照InVitro⽅式配制澄的储备液，再依次添加助溶剂：(为保证实验结果的可靠性，澄的储备液可以根据储存条件，适当保存；体内实验的⼯作液，建议您现⽤现配，当天使⽤；以下溶剂前显⽰的百分⽐指该溶剂在您配制终溶液中的体积占⽐；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的⽅式助溶)1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(7.81mM);Clearsolution1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(7.81mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(7.81mM);Clearsolution4.请依序添加每种溶剂：5%DMSO>>40%PEG300>>5%Tween-80>>50%salineSolubility:≥1.25mg/mL(3.90mM);Clearsolution5.请依序添加每种溶剂：5%DMSO>>95%(20%SBE-β-CDinsaline)Solubility:≥1.25mg/mL(3.90mM);Clearsolution6.请依序添加每种溶剂：PBSSolubility:220mg/mL(686.94mM);Clearsolution;NeedultrasonicBIOLOGICALACTIVITY⽣物活性Y-27632dihydrochloride⼀种具有⼝服活性的、ATP竞争性的ROCK(Rho-kinase)抑制剂(ROCK-IKi=220nM;ROCK-IIKi=300nM)。Y-27632dihydrochloride表现出抗癫痫的作⽤。IC50&TargetROCK-IROCK-IIPKNCitronkinase220nM(Ki)300nM(Ki)3.1μM(Ki)5.3μM(Ki)PKCαPKA73μM(Ki)25μM(Ki)体外研究Y-27632(1-5μM;0-60min)promotesneuronaldifferentiationofadiposetissue-derivedstemcells(ADSCs)[3].Y-27632(1-5μM;0-60min)inducestheexpressionofNSE,MAP-2andnestininADSCs[3].WesternBlotAnalysis[3]CellLine:Adiposetissue-derivedstemcells(ADSCs)Concentration:20μMIncubationTime:24hoursResult:Resultedintheup-regulationofNSE,MAP-2andnestinproteinlevelsby25.3,3.1and2.5fold,respectively,comparedtocontrolcellsnottreatedbyY-27632.体内研究Y-27632(oralgavage;30mg/kg;oncedaily;4w)preventsdimethylnitrosamine-inducedhepaticfibrosisinrats[1].Y-27632(oralgavage;5-10mg/kg;once)showsantiepilepticeffectsinepilepsyinducedbyPTZandMES[2].AnimalModel:MaleWistarratsinjectedwithdimethylnitrosamine[1]2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEDosage:30mg/kgAdministration:Oralgavage;30mg/kg;oncedaily;4weeksResult:Decreasedtheoccurrenceofdimethylnitrosamine-inducedhepaticfibrosisandreducedthecollagenandhydroxyprolinecontentandα-smoothmuscleactinexpressionintheliver.AnimalModel:MaleSwissalbinomiceinjectedwithPTZ(pentylenetetrazole)orinducedbyMES(maximalelectroconvulsiveshock)[2]Dosage:5-10mg/kgAdministration:Oralgavage;5-10mg/kg;onceResult:Prolongedtheonsettimeofmyoclonicjerkswhencomparedwiththoseobservedinthesalinegroup(P<0.05).Prolongedtheonsettimeofclonicconvulsionswhencomparedwithsalinegroup(P<0.05).Preventedtheoccurrenceoftonichindlimbextensionsanddeath.户使⽤本产品发表的科研⽂献•Nature.2022Nov;611(7936):603-613.•Nature.2022Jan;601(7894):600-605.•Science.2020Dec4;370(6521):eaay2002.•Immunity.2022Mar15;S1074-7613(22)00124-8.•CellDiscov.2022Apr19;8(1):35.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].TadaS,etal.AselectiveROCKinhibitor,Y27632,preventsdimethylnitrosamine-inducedhepaticfibrosisinrats.JHepatol.2001Apr;34(4):529-36.[2].InanS,etal.AntiepilepticeffectsoftwoRho-kinaseinhibitors,Y-27632andfasudil,inmice.BrJPharmacol.2008Sep;155(1):44-51.[3].XueZW,etal.Rho-associatedcoiledkinaseinhibitorY-27632promotesneuronal-likedifferentiationofadulthumanadiposetissue-derivedstemcells.ChinMedJ(Engl).2012Sep;125(18):3332-5.[4].IshizakiT,etal.PharmacologicalpropertiesofY-27632,aspecificinhibitorofrho-associatedkinases.MolPharmacol.2000May;57(