Zanapezil-TAK-147--生命科学试剂-MCE.pdf

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Zanapezil

Cat.No.:HY-19651A

CASNo.:142852-51-5

Synonyms:TAK-147

分⼦式:C₂₉H₃₆N₂O₅

分⼦量:492.61

作⽤靶点:Cholinesterase(ChE)

作⽤通路:NeuronalSignaling

储存⽅式:Pleasestoretheproductundertherecommendedconditionsin

theCertificateofAnalysis.

BIOLOGICALACTIVITY

⽣物活性Zanapezil(TAK-147)是⼀种有效、可逆和选择性的⼄酰胆碱酯酶(AChE)抑制剂。Zanapezil有效抑制⼤⿏⼤

脑⽪层匀浆中AChE活性(IC50=51.2nM)。Zanapezil适度抑制毒蕈碱M1和M2受体，Ki值分别为234和

340nM。Zanapezil可⽤于阿尔茨海默症早期阶段的研究[1]。

IC50TargetAChE

体外研究Zanapezil(TAK-147)showsapotentandreversibleinhibitionofAChEactivityinhomogenatesoftherat

cerebralcortex(IC50=51.2nM),andis3.0-and2.4-foldmorepotentthantacrineandphysostigmine,

respectively.Zanapezilistheleastpotentinhibitorofbutyrylcholinesteraseactivityinratplasma

(IC50=23,500nM)[1].

ZanapezilmoderatelyinhibitsuptakeofnoradrenalineandserotoninwithIC50valuesof4020and1350nM,

respectively[1].

Zanapezilalsoinhibitsligandbindingatalpha-1,alpha-2andserotonin2receptorswithKivaluesof324,

2330and3510nM,respectively[1].

体内研究