Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Zanapezil (TAK-147) is a powerful and selective inhibitor of acetylcholine esterase (AChE). It demonstrates significant and reversible inhibition of AChE activity in rat cerebral cortex homogenates (IC50 = 51.2 nM). Furthermore, Zanapezil exhibits moderate inhibition of muscarinic M1 and M2 receptor binding with Ki values of 234 and 340 nM, respectively. This compound holds promise for the investigation of the initial stages of Alzheimer's disease (AD).
产品描述 | Zanapezil (TAK-147) is a powerful and selective inhibitor of acetylcholine esterase (AChE). It demonstrates significant and reversible inhibition of AChE activity in rat cerebral cortex homogenates (IC50 = 51.2 nM). Furthermore, Zanapezil exhibits moderate inhibition of muscarinic M1 and M2 receptor binding with Ki values of 234 and 340 nM, respectively. This compound holds promise for the investigation of the initial stages of Alzheimer's disease (AD). |
体外活性 | Zanapezil (TAK-147) free base shows a potent and reversible inhibition of AChE activity in homogenates of the rat cerebral cortex (IC 50 =51.2 nM), and is 3.0- and 2.4-fold more potent than tacrine and physostigmine, respectively. Zanapezil free base is the least potent inhibitor of butyrylcholinesterase activity in rat plasma (IC 50 =23,500 nM)[1]. Zanapezil free base moderately inhibits uptake of noradrenaline and serotonin with IC 50 values of 4020 and 1350 nM, respectively[1]. Zanapezil free base also inhibits ligand binding at alpha-1, alpha-2 and serotonin 2 receptors with K i values of 324, 2330 and 3510 nM, respectively[1]. |
体内活性 | Oral administration of Zanapezil (TAK-147; 3 mg/kg) free base significantly accelerated the turnover rates of dopamine, noradrenaline and serotonin in the rat brain. Oral administration of Zanapezil free base at doses ranging from 1 to 10 mg/kg induces a statistically significant and dose-dependent decrease in AChE activity in the cerebral cortex in ex vivo experiments[1]. Zanapezil (TAK-147; 5 and 10 mg/kg) free base significantly increases ACh level in the ventral hippocampus (VH) for 120 min[2]. Animal Model: Male Wistar rats 7 weeks in age (230-240 g)[2]Dosage: 5 and 10 mg/kg Administration: Oral administration Result: Increased acetylcholine (ACh) level in the VH for 120 min. |
别名 | TAK-147 free base, Zanapezil free base |
分子量 | 376.544 |
分子式 | C25H32N2O |
CAS No. | 142852-50-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
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