Tacrine-hydrochloride-DataSheet-生命科学试剂-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•Agonists•ScreeningLibrarieswww.MedChemETacrinehydrochlorideCat.No.:HY-B1488CASNo.:1684-40-8分⼦式:C₁₃H₁₅ClN₂分⼦量:234.72作⽤靶点:AChE;iGluR作⽤通路:NeuronalSignaling;MembraneTransporter/IonChannel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H2O:83.33mg/mL(355.02mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM4.2604mL21.3020mL42.6040mL5mM0.8521mL4.2604mL8.5208mL10mM0.4260mL2.1302mL4.2604mL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，并请注意储备液的保存⽅式和期限。BIOLOGICALACTIVITY⽣物活性Tacrinehydrochloride⼀种AChE和BChE的有效抑制剂，IC50值分别为31nM和25.6nM。Tacrinehydrochloride也NMDAR的抑制剂，IC50值为26μM。Tacrinehydrochloride可⽤于研究阿尔茨海默⽒症。IC50&TargetIC50:31nM(AChE),25.6nM(BChE),26μM(NMDAR)[1][2]体外研究Tacrine(12.5-37.5nM)inhibitsvenomacetylcholinesteraseaswellashumanserumbutyrylcholinesteraseinaconcentration-dependentmanner[1].1/2MasterofSmallMolecules—您⾝边的抑制剂⼤师www.MedChemETacrinereducestheneurotoxicityinducedbytheactivationoftheNMDARsinmurinecorticalneuronalcultureswithanIC50of~500μM[2].TacrineinhibitstheNMDARresponsesinaconcentration-dependentmannerwithanIC50of~190μMat-60mV[2].体内研究Tacrine(20-40μmol/kg;s.c.)disruptsretentionoflearningin17-and30-dayoldmiceinpassiveavoidance,andwhilethelowdoseoftacrinetreatment(5μmol/kg;s.c.)improvesretentionin17-dayoldmice[2].Tacrine(0.1-0.4mg/mL;i.p.for7d)inhibitstheexpressionofAChE,butdoesnotsignificantlyimprovetheprotectionoftheretinafunctionandmorphologyinmice[3].REFERENCES[1].AhmedM,et,al.Inhibitionoftwodifferentcholinesterasesbytacrine.ChemBiolInteract.2006Aug25;162(2):165-71.c[2].HorakM,et,al.ThepharmacologyoftacrineatN-methyl-d-aspartatereceptors.ProgNeuropsychopharmacolBiolPsychiatry.2017Apr3;75:54-62.[3].Theprotectiveroleoftacrineanddonepezilintheretinaofacetylcholinesteraseknockoutmice.YiYM,et,al.IntJOphthalmol.2015Oct18;8(5):884-90.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseo