Thioacetamide-Acetothioamide-DataSheet-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEThioacetamideCat.No.:HY-Y0698CASNo.:62-55-5Synonyms:Acetothioamide;TAA;Thiacetamide分⼦式:C₂H₅NS分⼦量:75.13作⽤靶点:Necroptosis作⽤通路:Apoptosis储存⽅式:4°C,storedundernitrogen*Insolvent:-80°C,6months;-20°C,1month(storedunder

nitrogen)溶解性数据体外实验DMSO:100mg/mL(1331.03mM;Needultrasonic)H2O:50mg/mL(665.51mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM13.3103mL66.5513mL133.1026mL5mM2.6621mL13.3103mL26.6205mL10mM1.3310mL6.6551mL13.3103mL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(storedundernitrogen)。-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%saline1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.5mg/mL(33.28mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(33.28mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(33.28mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Thioacetamide(TAA)⼀种间接的肝毒素，可引起实质细胞坏死。Thioacetamide通过微粒体CYP2E1代谢激活最初为硫代⼄酰胺-S-氧化物，然后再转化为硫代⼄酰胺-S-⼆氧化物，这⼀种⾼度活性的代谢物，其活性代谢物与蛋⽩质和脂质共价结合，从⽽引起氧化应激和⼩叶中央坏死。Thioacetamide可诱发慢性肝纤维化、脑病等事件模型。体外研究Thioacetamide(TAA;0-10000μM;24h;WB-F344cells)hascytotoxicityinaconcentration-dependentmanner[4].Thioacetamide(TAA;1000and10000μM;0-24h;WB-F344cells)hasdifferentially-expressedgenesintheearlyphasesatlow(1000μM)andhigh(10000μM)concentrations[4].CellViabilityAssay[4]CellLine:WB-F344cellsConcentration:0-10000μMIncubationTime:24hoursResult:Had20%and50%celldeathatthe1000and10000μMconcentrations,respectively.体内研究Thioacetamide(TAA;100mg/kg;i.p.;threetimesweekly)caninducechronicliverfibrosisinmaleICRmice[2].Thioacetamide(200-1200mg/kg;i.p.;once)induceshepaticencephalopathymodelinC57BL/6mice[3].AnimalModel:MaleICRmice[2]Dosage:100mg/kgAdministration:Intraperitonealinjection;threetimesweeklyforeightweeksResult:InducedchronicliverfibrosisinmaleICRmiceandresultedinlowerbodyweight,serumcholesterolandtriglyceridesaswellasincreasedliversize,ALT,ASTandLDHvalues.AnimalModel:MaleC57BL/6mice(20-25g,aged8-12weeks)[3]Dosage:200,600,and1,200mg/kg2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEAdministration:Intraperitonealinjection;onceResult:Alteredtheneuropsychiatricstate,motorbehaviorandreflexandsensoryfunctions.IncreasedintheglutamatereleaseinthecerebralcortexofHepaticencephalopathy(HE)mice.REFERENCES[1].WallaceMC,et,al.Standardoperatingproceduresinexperimentalliverresearch:thioacetamidemodelinmiceandrats.LabAnim.2015Apr;49(1Suppl):21-9.[2].ChenIS,et,al.Hepatoprotectionofsilymarinagainstthioacetamide-inducedchronicliverfibrosis.JSciFoodAgric.2012May;92(7):1441-7.[3].MirandaAS,et,al.Athioacetamide-inducedhepaticencephalopathymodelinC57BL/6mice:abehavioralandneurochemicalstudy.ArqNeuropsiquiatr.2010Aug;68(4):597-602.[4].YeomHJ,et,al.Expressionanalysisofearlyresponse-relatedgenesinratliverepithelialcellsexposedtothioacetamideinvitro.JVetMedSci.2009Jun;71(6):719-27.McePdfHeightCaution:Producthas