Zanapezil free base T38895
品牌 | 厂商性质 | 产地 | 货期 |
---|---|---|---|
TargetMol | 生产商 | 美国 | 现货 |
性能特点
生化试剂,可用于动物细胞实验
规格 | CAS号 | 价格 | 操作 |
---|---|---|---|
25 mg | 142852-50-4 | ¥6,620.00 | 询底价 |
Product Introduction
Bioactivity
英文名: Zanapezil free base
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.
存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year
关键字: TAK147 | Zanapezil | TAK-147 | TAK 147
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