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Donepezil HCl
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Donepezil HCl图片
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
1g电议
5g电议

产品介绍
Donepezil HCl (E2020) 是一种可逆的选择性 AChE 抑制剂,对 AChE 活性的 IC50 为 6.7 nM。

Cell lines

Human SHSY5Y neuroblastoma cells, human umbilical vein endothelial cells

Preparation method

Limited solubility. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

1 h

Applications

Donepezil dose-dependently inhibited the carbachol-stimulated increase in intracellular Ca2+ concentration in human SHSY5Y neuroblastoma cells with the IC50 of 4.0 ± 0.2 μM. Donepezil protected human umbilical vein endothelial cells (HUVECs) against H2O2-induced cell injury. Donepezil (100 μM) decreased cell viability. Pretreatment with donepezil at concentrations of 1 and 10 μM significantly inhibited the H2O2–induced reduction in cell viability. Exposure of HUVECs to donepezil (1 μM) for 2 h upregulated HIF-1α expression.

Animal models

Male Lister Hooded rats, adult male NMRI mice

Dosage form

Intraperitoneal administration, 1 mg/kg

Application

In Male Lister Hooded rats, donepezil dose-dependently increased salivation and tremor with an ED50 of 6 μmol/kg. In adult male NMRI mice, donepezil (1 mg/kg) improved recognition performances.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

产品描述

Donepezil Hydrochloride (Donepezil HCL) is a novel, potent and selective inhibitor of acetylcholinesterase (AChE), an enzyme possibly involved in cognitive dysfunction of patients suffering Alzheimer’s disease (AD), with the half maximal inhibition concentration IC50 value of 6.7 nM [1].

Donepezil HCL is a piperidine-class AChE inhibitor containing an N-benzylpiperdine and an indanone moiety, which confers it a longer and more selective action against AchE as compared to BuChE (IC50: 7.4 μM) [1].

Donepezil HCL has been approved by FDA for the treatment of AD, in which it has improved cognitive function of mild to severe moderate AD patients and exhibited excellent tolerability without hepatotoxicity [1].

Reference

References:
[1] Sugimoto H, Ogura H, Arai Y, Limura Y, Yamanishi Y. Research and development of donepezil hydrochloride, a new type of acetylcholinesterase inhibitor. Jpn J Pharmacol. 2002 May;89(1):7-20.