Cystamine-dihydrochloride-DataSheet-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemECystamine(dihydrochloride）Cat.No.:HY-W020050CASNo.:56-17-7分⼦式:C₄H₁₄Cl₂N₂S₂分⼦量:225.2作⽤靶点:Caspase;Glutaminase;Apoptosis作⽤通路:Apoptosis;MetabolicEnzyme/Protease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DMSO:100mg/mL(444.05mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM4.4405mL22.2025mL44.4050mL5mM0.8881mL4.4405mL8.8810mL10mM0.4440mL2.2202mL4.4405mL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(11.10mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.5mg/mL(11.10mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(11.10mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Cystamine(dihydrochloride)游离硫醇半胱胺的⼆硫化物形式。Cystamine⼀种转⾕氨酰胺酶(Tgase)抑制剂，具有⼝服活性。Cystamine对caspase-3也有抑制活性，IC50值为23.6μM。Cystamine可⽤于亨廷顿舞蹈病（HD）等多种疾病的研究。IC50&TargetCaspase323.6μM(IC50)体外研究Cystamine(dihydrochloride)hasinhibitionactivityforcaspase-3withanIC50valueof23.6μM[1].Cystamine(0-500μM;0-16h)inhibitsrecombinantactivecaspase-3inaconcentration-dependentmanner[1].Cystamine(250μM;10h)robustlyincreasesthelevelsofglutathione[1].WesternBlotAnalysis[1]CellLine:HumanneuroblastomaSH-SY5YcellsConcentration:250,500μMIncubationTime:0-16hResult:InhibitedtheMG132-mediatedactivationofcaspase-3.InhibitedtheH2O2-mediatedactivationofcaspase-3.Inhibitedcaspase-3activityinatTG-independentmanner.体内研究Cystamine(dihydrochloride)(oral,i.p.;112,225mg/kg)reducesTgaseactivityandGGELlevels,lessensthebehavioralandneuropathologicalseverity,andextendssurvivalinR6/2transgenicHDmice[2].AnimalModel:R6/2transgenicHDmice[2]Dosage:112,225mg/kgAdministration:Intraperitonealororal,dailyResult:Significantlyextendedsurvival,improvedbodyweightandmotorperformance,delayedtheneuropathologicalsequelaandsignificantlyalteredthelevelsofTgaseactivityandN(Sigma)-(gamma-L-glutamyl)-L-lysine(GGEL)levels.REFERENCES2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE[1].MathieuLesort,etal.Cystamineinhibitscaspaseactivity.Implicationsforthetreatmentofpolyglutaminedisorders.JBiolChem.2003Feb7;278(6):3825-30.[2].AlpaslanDedeoglu,etal.TherapeuticeffectsofcystamineinamurinemodelofHuntington'sdisease.JNeurosci.2002Oct15;22(20):8942-50.[3].ThomasMJeitner,etal.Cystamineandcysteamineasinhibitorsoftransglutaminaseactivityinvivo.BiosciRep.2018Sep5;38(5):BSR20180691.McePdfHeightCaution:Producthasnotbeenfullyvali