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

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemETacrinehydrochloride(hydrate)Cat.No.:HY-B2244CASNo.:206658-92-6分⼦式:C₁₃H₁₄N₂.xHCl.xH₂O作⽤靶点:Cholinesterase(ChE)作⽤通路:NeuronalSignaling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(Needultrasonic)DMSO:32mg/mL(Needultrasonicandwarming)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(InfinitymM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(InfinitymM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(InfinitymM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Tacrinehydrochloride(hydrate)⼄酰胆碱酯酶(AChE)和丁酰胆碱酯酶(BChE)的抑制剂，其IC50值分别为31nM和25.6nM。1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEIC50&TargetIC50:31nM(AChE),25.6nM(BChE)体外研究Tacrinehydrochloride(hydrate)(12.5to37.5nM)inhibitsvenomacetylcholinesteraseaswellashumanserumbutyrylcholinesteraseinaconcentration-dependentmanner.TheIC50is31nMforsnakevenomAChEand25.6nMforhumanBChE[1].体内研究PretreatmentwithTacrinehydrochloride(hydrate)alsomodifiesabsolutelevelsofcocaineself-administrationduringreacquisition.Bodyweightdeclinesapproximatelyone-halfpercentoverfourdaysoftreatmentwithintravenousTacrinehydrochloride(hydrate).DeliveryofTacrinehydrochloride(hydrate)byosmoticpumpdoesnotaltereitherlinear-orrepeated-cocaine-inducedlocomotoractivity.ThereisnosignificantmaineffectorinteractionwithTacrinehydrochloride(hydrate)treatmentonactiveleverrespondingduringreinstatement.Posthoccomparisonsindicatethatratsself-administeringcocainehassignificantlyloweralkalinephosphataselevels,relativetoTTacrinehydrochloride(hydrate)-butnotsaline-treatedratsevaluatedbyconditioned-placepreference[2].PROTOCOLKinaseAssay[1]ThekineticparametersoftheinteractionbetweenTacrinehydrochloridehydrateandcholinesterasearedeterminedusingthedoublereciprocalplotanalyzedoverarangeofacetylthiocholineconcentrations(0.05to1mM)intheabsenceandinthepresenceofTacrinehydrochloridehydrate(12.5to37.5nM).IC50isdeterminedbypercentageresidualactivityversusconcentrationofTacrinehydrochloridehydrate[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.AnimalMaleWistarratsat9weeksofageareusedinthisstudy.Assoonasratsexhibitastablepatternofself-Administration[2]administrationunderfixed-ratio-5(FR-5)witha20-secondtimeout,sessionsarediscontinuedover24hoursandratsareleftundisturbedinhomecages,attachedtoafluidswivelandsteel-coiltether.Thisinitialwashoutintervalisassessedasmorethanadequatetoallowclearanceofplasmacocaine,whichhasahalf-lifeoflessthan20minutesinrats.Beginningonthefollowingday,10mg/kg-dayofTacrinehydrochloridehydrateorvehicle(saline)isadministeredasachronicinfusionover4days,deliveredintravenouslyat4.0mlperday.Aftercompletionoftheseinfusions,ratsarethenleftundisturbedinhomecagesforanadditionaltwodays.ThissecondwashoutperiodpermitscompleteclearanceofTacrinehydrochloridehydrate,whichhasahalf-lifeoflessthantwohoursinratbrain.Cocaineself-administrationisthenre-initiatedunderFR-5witha20-secondtime-outperiod.TodeterminepersistenteffectsofTacrinehydrochloridehydrate,thepatternofself-administrationismonitoredoversixadditionalsessions[2].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.户使⽤本产品发表的科研⽂献•CellDeathDis.2022Jan10;13(1):48.Seemorecustomervalidationsonwww.MedChemEREFERENCES2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE[1].AhmedM,etal.Inhibitionoftwodifferentcholinesterasesbytacrine.ChemBiolInteract.2006Aug25;162(2):165-71.[2].GrasingK,etal.Enduringeffectsoftacrineoncocaine-reinforcedbehavior:Analysisbyconditioned-placepreference,temporalseparationfromdrugreward,andreinstatement.Pharmaco