Donepezil HCl

目录号: GC14490纯度: >99.50%同义词: 盐酸多奈哌齐; E2020

An AChE inhibitor


Donepezil HCl
Cas No.: 120011-70-3
规格价格库存数量操作
1g¥557.00现货
1
5g¥1,670.00现货
1
10mM (in 1mL DMSO)¥378.00现货
1

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产品描述 Description

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].

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.

实验参考方法 Experimental Reference Method

Cell experiment [1,2]:

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 experiment [1,3]:

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.

References:

[1]. Snape M F, Misra A, Murray T K, et al. A comparative study in rats of the in vitro and in vivo pharmacology of the acetylcholinesterase inhibitors tacrine, donepezil and NXX-066[J]. Neuropharmacology, 1999, 38(1): 181-193.

[2]. Huang Z H, Guo W, Zhang L L, et al. Donepezil protects endothelial cells against hydrogen peroxide‐induced cell injury[J]. CNS neuroscience & therapeutics, 2012, 18(2): 185-187.

[3].Freret T, Bouet V, Quiedeville A, et al. Synergistic effect of acetylcholinesterase inhibition (donepezil) and 5-HT 4 receptor activation (RS67333) on object recognition in mice[J]. Behavioural brain research, 2012, 230(1): 304-308.

产品文档 Product Documents

Purity:>99.50%

化学性质Chemical Properties

CAS 号
120011-70-3
同义词
盐酸多奈哌齐; E2020
化学名
2-[(1-benzylpiperidin-4-yl)methyl]-5,6-dimethoxy-2,3-dihydroinden-1-one;hydrochloride
SMILES
COC1=C(C=C2C(=C1)CC(C2=O)CC3CCN(CC3)CC4=CC=CC=C4)OC.Cl
分子式
C24H30ClNO3
分子量
415.95 g/mol
溶解性
≥ 10.4mg/mL in Water
保存条件
Store at -20°C
General tips
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 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至 37°C,然后在超声波浴中震荡一段时间。
Shipping Condition
评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备 RT,或根据请求配备蓝冰。

计算工具摩尔浓度 / 稀释 / 分子量 / 单位换算 / 体内配方 / 溶解度

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