Y-27632-dihydrochloride-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEY-27632dihydrochlorideCat.No.:HY-10583CASNo.:129830-38-2分?式:C??H??Cl?N?O分?量:320.26作?靶點:ROCK作?通路:CellCycle/DNADamage;Cytoskeleton;StemCell/Wnt;TGF-beta/Smad儲存?式:4°C,sealedstorage,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoisture)溶解性數(shù)據(jù)體外實驗H2O:100mg/mL(312.25mM;Needultrasonic)DMSO:33.33mg/mL(104.07mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM3.1225mL15.6123mL31.2246mL5mM0.6245mL3.1225mL6.2449mL10mM0.3122mL1.5612mL3.1225mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；?旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month(sealedstorage,awayfrommoisture)。-80°C儲存時，請在6個?內(nèi)使?，-20°C儲存時，請在1個?內(nèi)使?。體內(nèi)實驗請根據(jù)您的實驗動物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：(為保證實驗結(jié)果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實驗的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)天使?；以下溶劑前顯?的百分?指該溶劑在您配制終溶液中的體積占?；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的?式助溶)1.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(7.81mM);Clearsolution1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(7.81mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(7.81mM);Clearsolution4.請依序添加每種溶劑：5%DMSO>>40%PEG300>>5%Tween-80>>50%salineSolubility:≥1.25mg/mL(3.90mM);Clearsolution5.請依序添加每種溶劑：5%DMSO>>95%(20%SBE-β-CDinsaline)Solubility:≥1.25mg/mL(3.90mM);Clearsolution6.請依序添加每種溶劑：PBSSolubility:220mg/mL(686.94mM);Clearsolution;NeedultrasonicBIOLOGICALACTIVITY?物活性Y-27632dihydrochloride?種具有?服活性的、ATP競爭性的ROCK(Rho-kinase)抑制劑(ROCK-IKi=220nM;ROCK-IIKi=300nM)。Y-27632dihydrochloride表現(xiàn)出抗癲癇的作?。IC50&TargetROCK-IROCK-IIPKNCitronkinase220nM(Ki)300nM(Ki)3.1μM(Ki)5.3μM(Ki)PKCαPKA73μM(Ki)25μM(Ki)體外研究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.體內(nèi)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?邊的抑制劑?師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.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?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(