Donepezil (Synonyms: 多奈哌齐; E2020 free base)

目录号: HY-14566 纯度: 99.91%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

Donepezil (E2020 free base) 是 AChE 抑制剂，对牛 AChE 和人 AChE 的 IC₅₀ 分别为 8.12 nM 和 11.6 nM。

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Donepezil Chemical Structure

CAS No. : 120014-06-4

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥500	In-stock
1 mg	￥140	In-stock
5 mg	￥281	In-stock
10 mg	￥450	In-stock
50 mg	￥1004	In-stock
100 mg	￥1786	In-stock
200 mg		询价
500 mg		询价

or 大包装询价

* Please select Quantity before adding items.

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MCE 顾客使用本产品发表的 9 篇科研文献

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AChE BChE

生物活性
纯度 & 产品资料
参考文献

生物活性

Donepezil (E2020 free base) is a specific and potent AChE inhibitor with IC₅₀s of 8.12 nM and 11.6 nM for bovine AChE and human AChE, respectively^[1].

IC₅₀ & Target

AChE

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
BV-2	IC₅₀	1.54 μM Compound: Donepezil	Cytotoxicity against mouse BV-2 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay Cytotoxicity against mouse BV-2 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay	[PMID: 34923430]
CHO	IC₅₀	34.3 μM Compound: donepezil	Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits	[PMID: 23812503]
HEK293	IC₅₀	> 200 μM Compound: Donepezil	Cytotoxicity against human HEK293 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Cytotoxicity against human HEK293 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 32388114]
HEK293	IC₅₀	0.009 μM Compound: 1	Inhibition of human recombinant AChE expressed in HEK293 cells using acetylthiocholine iodide as substrate preincubated for 30 mins followed by substrate addition measured after 30 mins by Ellman's method Inhibition of human recombinant AChE expressed in HEK293 cells using acetylthiocholine iodide as substrate preincubated for 30 mins followed by substrate addition measured after 30 mins by Ellman's method	[PMID: 26471320]
HEK293	IC₅₀	0.01 μM Compound: Donepezil	Inhibition of recombinant human AChE expressed in HEK293 cells using acetylthiocholine iodide as substrate pretreated for 5 mins followed by substrate addition measured for 5 mins by UV-Vis spectrophotometric method Inhibition of recombinant human AChE expressed in HEK293 cells using acetylthiocholine iodide as substrate pretreated for 5 mins followed by substrate addition measured for 5 mins by UV-Vis spectrophotometric method	[PMID: 28242552]
HEK293	IC₅₀	0.016 μM Compound: donepezil	Inhibition of recombinant human AChE expressed in HEK293 cells preincubated for 15 mins Inhibition of recombinant human AChE expressed in HEK293 cells preincubated for 15 mins	[PMID: 25418133]
HEK293	IC₅₀	6.2 nM Compound: Donepezil	Inhibition of human recombinant AChE expressed in HEK293 cells using acetylthiocholine iodide as substrate by Ellman's method Inhibition of human recombinant AChE expressed in HEK293 cells using acetylthiocholine iodide as substrate by Ellman's method	[PMID: 31304000]
HEK293	IC₅₀	7.5 μM Compound: 1	Inhibition of human recombinant BuChE expressed in HEK293 cells using S-butyrylthiocholine iodide as substrate preincubated for 30 mins followed by substrate addition measured after 30 mins by Ellman's method Inhibition of human recombinant BuChE expressed in HEK293 cells using S-butyrylthiocholine iodide as substrate preincubated for 30 mins followed by substrate addition measured after 30 mins by Ellman's method	[PMID: 26471320]
HEK293	IC₅₀	8.2 μM Compound: donepezil	Inhibition of recombinant human BuChE expressed in HEK293 cells preincubated for 15 mins Inhibition of recombinant human BuChE expressed in HEK293 cells preincubated for 15 mins	[PMID: 25418133]
HepG2	IC₅₀	262727 nM Compound: Donepezil	Cytotoxicity against human HepG2 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay Cytotoxicity against human HepG2 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay	[PMID: 34530383]
HFF	IC₅₀	0.091 μM Compound: Donepezil	Cytotoxicity against HFF cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Cytotoxicity against HFF cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 32088494]
HT-22	IC₅₀	56.42 μM Compound: Donepezil	Cytotoxicity against mouse HT-22 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay Cytotoxicity against mouse HT-22 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay	[PMID: 34923430]
MCF7	IC₅₀	0.06 μM Compound: Donepezil	Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay	[PMID: 32088494]
NIH3T3	IC₅₀	316.42 μM Compound: Donepezil	Cytotoxicity against mouse NIH/3T3 cells after 24 hrs by MTT assay Cytotoxicity against mouse NIH/3T3 cells after 24 hrs by MTT assay	[PMID: 27789142]
SH-SY5Y	IC₅₀	> 200 μM Compound: Donepezil	Cytotoxicity against human SH-SY5Y cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Cytotoxicity against human SH-SY5Y cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 32388114]
SH-SY5Y	IC₅₀	0.3 μM Compound: Donepezil	Cytotoxicity against human SH-SY5Y cells measured after 48 hrs by MTT assay Cytotoxicity against human SH-SY5Y cells measured after 48 hrs by MTT assay	[PMID: 32088494]
SH-SY5Y	IC₅₀	15.54 μM Compound: 1	Cytotoxicity against human SH-SY5Y cells after 72 hrs by SRB assay Cytotoxicity against human SH-SY5Y cells after 72 hrs by SRB assay	[PMID: 27823887]
SH-SY5Y	IC₅₀	155 μM Compound: 2; Don	Antialzheimer activity in human SH-SY5Y cells assessed as inhibition of GA-induced tau hyperphosphorylation at Ser396 residue incubated for 24 hrs by ELISA Antialzheimer activity in human SH-SY5Y cells assessed as inhibition of GA-induced tau hyperphosphorylation at Ser396 residue incubated for 24 hrs by ELISA	[PMID: 36257284]
SH-SY5Y	IC₅₀	202 μM Compound: 2; Don	Antioxidant activity against okadaic acid-induced ROS generation in human SH-SY5Y cells assessed as reduction in DCF fluorescence intensity pretreated for 24 hrs followed by okadaic acid addition for 24 hrs by DCFH-DA dye based fluorescence analysis Antioxidant activity against okadaic acid-induced ROS generation in human SH-SY5Y cells assessed as reduction in DCF fluorescence intensity pretreated for 24 hrs followed by okadaic acid addition for 24 hrs by DCFH-DA dye based fluorescence analysis	[PMID: 36257284]
SH-SY5Y	CC₅₀	25.06 μM Compound: Donepezil	Cytotoxicity in human SH-SY5Y cells assessed as reduction in cell viability after 72 hrs incubation by MTT assay Cytotoxicity in human SH-SY5Y cells assessed as reduction in cell viability after 72 hrs incubation by MTT assay	[PMID: 30822710]
SH-SY5Y	IC₅₀	326 μM Compound: 2; Don	Neuroprotective activity in human SH-SY5Y cells assessed as inhibition of okadaic acid-induced mitochondrial membrane potential by measuring increase in red-to-green fluorescence intensity ratio pretreated for 24 hrs followed by okadaic acid addition for Neuroprotective activity in human SH-SY5Y cells assessed as inhibition of okadaic acid-induced mitochondrial membrane potential by measuring increase in red-to-green fluorescence intensity ratio pretreated for 24 hrs followed by okadaic acid addition for	[PMID: 36257284]
SH-SY5Y	IC₅₀	35 μM Compound: 2; Don	Antialzheimer activity in human SH-SY5Y cells assessed as inhibition of GA-induced tau hyperphosphorylation at Ser199 residue incubated for 24 hrs by ELISA Antialzheimer activity in human SH-SY5Y cells assessed as inhibition of GA-induced tau hyperphosphorylation at Ser199 residue incubated for 24 hrs by ELISA	[PMID: 36257284]
SH-SY5Y	IC₅₀	84.1 μM Compound: Donepezil	Neurotoxicity against human SH-SY5Y cells assessed as inhibition of cell viability incubated for 24 hrs by MTT assay Neurotoxicity against human SH-SY5Y cells assessed as inhibition of cell viability incubated for 24 hrs by MTT assay	[PMID: 30795991]
SH-SY5Y	IC₅₀	95.13 μM Compound: 1	Cytotoxicity against human SH-SY5Y cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay Cytotoxicity against human SH-SY5Y cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay	[PMID: 31280020]
SK-N-MC	IC₅₀	> 100 μM Compound: Donepezil	Antiproliferative activity against human SK-N-MC cells after 72 hrs by MTT assay Antiproliferative activity against human SK-N-MC cells after 72 hrs by MTT assay	[PMID: 28841514]

体外研究
(In Vitro)

Donepezil (E2020 free base) 以浓度依赖性方式抑制人 SHSY5Y 神经母细胞瘤细胞中卡巴胆碱刺激的细胞内 Ca2+ 浓度增加，表明 Donepezil 具有毒蕈碱拮抗剂活性。大鼠腹腔内给予 Donepezil 会导致流涎和震颤的剂量依赖性增加，这是明显的胆碱能行为体征，ED50 为 6 μMol/kg。口服给药后，发现 Donepezil 的 ED50 为 50 μMol/kg 效力稍差^[2]。
最近的一项研究表明，Donepezil 可以保护人脐静脉内皮细胞 (HUVEC) 免受 H2O2 诱导的细胞损伤。这可能有助于作为心脑血管疾病中氧化应激的潜在疗法^[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

分子量

379.49

Formula

C₂₄H₂₉NO₃

CAS 号

120014-06-4

性状

固体

颜色

White to off-white

中文名称

多奈哌齐

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

溶解性数据

细胞实验：

DMSO 中的溶解度 : 33.33 mg/mL (87.83 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.6351 mL	13.1756 mL	26.3512 mL
5 mM	0.5270 mL	2.6351 mL	5.2702 mL
10 mM	0.2635 mL	1.3176 mL	2.6351 mL

查看完整储备液配制表

* 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, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)。-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。

摩尔计算器
稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物实验：

请根据您的实验动物和给药方式选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.59 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水定容至 1 mL。
生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
方案二

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.59 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
方案三

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (6.59 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

请输入您的动物体内配方组成：

DMSO +

Tween-80 +

Saline

如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。

方案所需 助溶剂 包括：DMSO，，均可在 MCE 网站选购。，Tween 80，均可在 MCE 网站选购。

计算结果

工作液所需浓度 : mg/mL

储备液配制方法 : mg 药物溶于 μL DMSO（母液浓度为 mg/mL）。

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。

动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。

连续给药周期超过半月以上，请谨慎选择该方案。

请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热（超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。

纯度 & 产品资料

纯度: 99.91%

选择批次：

Data Sheet (640 KB) SDS (393 KB)

COA (285 KB) LCMS (107 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Ogura, H., et al., Comparison of inhibitory activities of donepezil and other cholinesterase inhibitors on acetylcholinesterase and butyrylcholinesterase in vitro. Methods Find Exp Clin Pharmacol, 2000. 22(8): p. 609-13. [Content Brief]

[2]. Snape, M.F., et al., A comparative study in rats of the in vitro and in vivo pharmacology of the acetylcholinesterase inhibitors tacrine, donepezil and NXX-066. Neuropharmacology, 1999. 38(1): p. 181-93. [Content Brief]

[3]. Huang, Z.H., et al., Donepezil protects endothelial cells against hydrogen peroxide-induced cell injury. CNS Neurosci Ther, 2012. 18(2): p. 185-7. [Content Brief]

Donepezil 相关分类

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.6351 mL	13.1756 mL	26.3512 mL	65.8779 mL
	5 mM	0.5270 mL	2.6351 mL	5.2702 mL	13.1756 mL
	10 mM	0.2635 mL	1.3176 mL	2.6351 mL	6.5878 mL
	15 mM	0.1757 mL	0.8784 mL	1.7567 mL	4.3919 mL
	20 mM	0.1318 mL	0.6588 mL	1.3176 mL	3.2939 mL
	25 mM	0.1054 mL	0.5270 mL	1.0540 mL	2.6351 mL
	30 mM	0.0878 mL	0.4392 mL	0.8784 mL	2.1959 mL
	40 mM	0.0659 mL	0.3294 mL	0.6588 mL	1.6469 mL
	50 mM	0.0527 mL	0.2635 mL	0.5270 mL	1.3176 mL
	60 mM	0.0439 mL	0.2196 mL	0.4392 mL	1.0980 mL
	80 mM	0.0329 mL	0.1647 mL	0.3294 mL	0.8235 mL

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Donepezil120014-06-4E2020多奈哌齐E 2020E-2020Cholinesterase (ChE)AChEbAChEhAChEInhibitorinhibitorinhibit

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Donepezil (Synonyms: 多奈哌齐; E2020 free base)

Customer Review

Other Forms of Donepezil:

MCE 顾客使用本产品发表的 9 篇科研文献

Donepezil 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

查看 Cholinesterase (ChE) 亚型特异性产品:

生物活性

纯度 & 产品资料

参考文献

摩尔计算器

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Donepezil 相关分类

完整储备液配制表

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Donepezil (Synonyms: 多奈哌齐; E2020 free base)

Customer Review

Other Forms of Donepezil:

Donepezil 相关抗体

MCE 顾客使用本产品发表的 9 篇科研文献

Donepezil 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

查看 Cholinesterase (ChE) 亚型特异性产品:

生物活性

纯度 & 产品资料

参考文献

Donepezil 相关抗体:

摩尔计算器

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Donepezil 相关分类

完整储备液配制表

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