Tacrine

目录号: HY-111338 纯度: 99.91%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

Tacrine 是一种可口服的有效的乙酰胆碱 (AChE) 抑制剂 (IC₅₀=109 nM)，同时也是一种 CYP1A2 底物活性分子。Tacrine 可恢复老年大鼠的认知功能障碍。Tacrine 可沉淀肝毒性并用于阿尔兹海默症的研究。

MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

Tacrine Chemical Structure

CAS No. : 321-64-2

1. 客户无需承担相应的运输费用。

2. 同一机构（单位）同一产品试用装仅限申领一次，同一机构（单位）一年内

可免费申领三个不同产品的试用装。

3. 试用装只面向终端客户。

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥880	In-stock
5 mg	￥800	In-stock
10 mg	￥1200	In-stock
50 mg	￥2800	In-stock
100 mg	￥4500	In-stock
500 mg	现货	询价
1 g		询价
5 g		询价

or 大包装询价

* Please select Quantity before adding items.

Customer Review

Other Forms of Tacrine:

Tacrine hydrochloride In-stock
Tacrine hydrochloride (hydrate) In-stock

MCE 顾客使用本产品发表的 5 篇科研文献

Tacrine 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:

查看所有亚型

AChE BChE

生物活性
纯度 & 产品资料
参考文献

生物活性

Tacrine is an effective oral acetylcholine (AChE) inhibitor (IC₅₀ = 109 nM) and also acts as an active substrate for CYP1A2. Tacrine can restore cognitive dysfunction in elderly rats. Tacrine can cause liver toxicity and is used in research related to Alzheimer's disease^[1]^[2]^[3]^[4].

IC₅₀ & Target

AChE

109 nM (IC₅₀)

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
A549	GI₅₀	> 100 μM Compound: Tacrine	Antiproliferative activity against human A549 cells after 48 hrs by SRB assay Antiproliferative activity against human A549 cells after 48 hrs by SRB assay	[PMID: 28728108]
C6	IC₅₀	450.7 μM Compound: Tacrine	Cytotoxicity against rat C6 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay Cytotoxicity against rat C6 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay	[PMID: 32904099]
Cerebral cortex neuron	EC₅₀	1.33 μM Compound: Tacrine	Neuroprotective activity in 20 uM rotenone and 10 uM oligomycin-treated Wistar rat primary cortical neurons assessed as increase in cell viability after 24 hrs by XTT assay Neuroprotective activity in 20 uM rotenone and 10 uM oligomycin-treated Wistar rat primary cortical neurons assessed as increase in cell viability after 24 hrs by XTT assay	[PMID: 22795665]
CHO-K1	IC₅₀	248 μM Compound: THA; 3	Cytotoxicity against CHOK1 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay Cytotoxicity against CHOK1 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay	[PMID: 30851693]
HBL-100	GI₅₀	50 μM Compound: Tacrine	Antiproliferative activity against human HBL100 cells after 48 hrs by SRB assay Antiproliferative activity against human HBL100 cells after 48 hrs by SRB assay	[PMID: 28728108]
HEK293	IC₅₀	0.13 μM Compound: Tacrine	Inhibition of recombinant human AChE expressed in HEK293 cells using acetylthiocholine iodide as substrate pretreated for 5 mins followed by substrate addition measured after 5 mins by spectrophotometry based Ellman method Inhibition of recombinant human AChE expressed in HEK293 cells using acetylthiocholine iodide as substrate pretreated for 5 mins followed by substrate addition measured after 5 mins by spectrophotometry based Ellman method	[PMID: 27918993]
HEK293	IC₅₀	0.15 μM Compound: Tacrine	Inhibition of recombinant human AChE expressed in HEK293 cells using acetylthiocholine iodide as substrate preincubated for 5 mins before substrate addition measured after 10 mins by Ellman's method Inhibition of recombinant human AChE expressed in HEK293 cells using acetylthiocholine iodide as substrate preincubated for 5 mins before substrate addition measured after 10 mins by Ellman's method	10.1039/C1MD00221J
HEK293	IC₅₀	122 nM Compound: Tacrine	Inhibition of cerebral human recombinant AchE expressed in HEK293 cells using acetylthiocholine iodide as substrate preincubated for 10 mins measured after 15 mins of substrate addition by Ellman's method Inhibition of cerebral human recombinant AchE expressed in HEK293 cells using acetylthiocholine iodide as substrate preincubated for 10 mins measured after 15 mins of substrate addition by Ellman's method	[PMID: 22023459]
HEK293	IC₅₀	21.72 μM Compound: Tacrine	Inhibition of human OCT1 expressed in HEK293 cells assessed as decrease in uptake of ASP+ after 2 mins by fluorescence assay Inhibition of human OCT1 expressed in HEK293 cells assessed as decrease in uptake of ASP+ after 2 mins by fluorescence assay	[PMID: 28230985]
HEK293	IC₅₀	412 nM Compound: 1	Inhibition of human recombinant AChE expressed in HEK293 cells using acetylcholine iodide as substrate preincubated with enzyme for 20 mins followed by substrate addition and measured after 5 mins by Ellman's method Inhibition of human recombinant AChE expressed in HEK293 cells using acetylcholine iodide as substrate preincubated with enzyme for 20 mins followed by substrate addition and measured after 5 mins by Ellman's method	[PMID: 31376562]
HeLa	GI₅₀	51 μM Compound: Tacrine	Antiproliferative activity against human HeLa cells after 48 hrs by SRB assay Antiproliferative activity against human HeLa cells after 48 hrs by SRB assay	[PMID: 28728108]
HepG2	IC₅₀	111 μM Compound: 1	Cytotoxicity against human HepG2 cells after 72 hrs by alamar blue assay Cytotoxicity against human HepG2 cells after 72 hrs by alamar blue assay	[PMID: 30108847]
HepG2	IC₅₀	114.9 μM Compound: Tacrine	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: 32904099]
HepG2	IC₅₀	144826 nM Compound: Tacrine	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]
HepG2	IC₅₀	168.47 μM Compound: THA	Cytotoxicity against human HepG2 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay Cytotoxicity against human HepG2 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay	[PMID: 33984470]
HepG2	IC₅₀	168.47 μM Compound: THA; Tacrine	Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 24 hrs by MTT assay Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 24 hrs by MTT assay	[PMID: 29533874]
HepG2	IC₅₀	17.9 μg/mL Compound: Tacrine	Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 24 hrs by MTT assay Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 24 hrs by MTT assay	[PMID: 28189905]
HepG2	EC₅₀	179 μM Compound: Tacrine	Hepatotoxicity in human HepG2 cells assessed as reduction in cell viability by MTT assay Hepatotoxicity in human HepG2 cells assessed as reduction in cell viability by MTT assay	[PMID: 27128182]
HepG2	IC₅₀	19.37 μM Compound: 1	Hepatotoxicity in human HepG2 cells assessed as cell viability after 24 hrs by MTT assay Hepatotoxicity in human HepG2 cells assessed as cell viability after 24 hrs by MTT assay	[PMID: 26503905]
HepG2	IC₅₀	190 μM Compound: THA; 3	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: 30851693]
HepG2	IC₅₀	98 μM Compound: Tacrine	Cytotoxicity against human HepG2 cell assessed as reduction in cell viability incubated for 72 hrs by MTT assay Cytotoxicity against human HepG2 cell assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 30771604]
HepG2	IC₅₀	98.73 μM Compound: Tacrine	Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay	[PMID: 24794747]
J774.1	IC₅₀	> 100 μM Compound: 1a	Cytotoxicity against mouse J774.1 cells after 24 hrs by alamar blue assay Cytotoxicity against mouse J774.1 cells after 24 hrs by alamar blue assay	[PMID: 28698054]
J774.1	IC₅₀	> 100 μM Compound: 1a; Tacrine	Cytotoxicity against mouse J774.1 cells after 24 hrs by AlamarBlue based cytotoxicity assay Cytotoxicity against mouse J774.1 cells after 24 hrs by AlamarBlue based cytotoxicity assay	[PMID: 27316542]
Primary neuron	IC₅₀	7.87 μM Compound: Tacrine	Toxicity in mouse neuronal cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Toxicity in mouse neuronal cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 30771604]
SH-SY5Y	IC₅₀	0.5 μM Compound: 1; THA	Inhibition of human SH-SY5Y cell lysate acetylcholinesterase using acetylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition by Ellman's method Inhibition of human SH-SY5Y cell lysate acetylcholinesterase using acetylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition by Ellman's method	[PMID: 30744931]
SH-SY5Y	IC₅₀	120 μM Compound: Tac	Cytotoxicity against human SH-SY5Y cells assessed as reduction in cell viability after 48 hrs by MTT assay Cytotoxicity against human SH-SY5Y cells assessed as reduction in cell viability after 48 hrs by MTT assay	[PMID: 29541355]
SW1573	GI₅₀	50 μM Compound: Tacrine	Antiproliferative activity against human SW1573 cells after 48 hrs by SRB assay Antiproliferative activity against human SW1573 cells after 48 hrs by SRB assay	[PMID: 28728108]
T47D	GI₅₀	46 μM Compound: Tacrine	Antiproliferative activity against human T47D cells after 48 hrs by SRB assay Antiproliferative activity against human T47D cells after 48 hrs by SRB assay	[PMID: 28728108]
Vero	IC₅₀	168.9 μM Compound: Tacrine	Cytotoxicity against monkey Vero cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay Cytotoxicity against monkey Vero cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay	[PMID: 32904099]
WiDr	GI₅₀	34 μM Compound: Tacrine	Antiproliferative activity against human WiDr cells after 48 hrs by SRB assay Antiproliferative activity against human WiDr cells after 48 hrs by SRB assay	[PMID: 28728108]

体内研究
(In Vivo)

Tacrine (0.3-3 mg/kg，口服，单次剂量) 增加大鼠海马细胞外乙酰胆碱水平，改善行为功能^[1]。

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

Animal Model:	6- and 22-24-month-old rats^[1]
Dosage:	0.3, 1, 3 mg/kg; single dose
Administration:	Oral
Result:	Doubled the extracellular acetylcholine levels in young rats' hippocampal cells and increased it six times in older rats, improving discrimination ability, restoring passive avoidance conditioning responses, and enhancing behavioral function.

Clinical Trial

分子量

198.26

Formula

C₁₃H₁₄N₂

CAS 号

321-64-2

性状

固体

颜色

Off-white to light yellow

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 : ≥ 100 mg/mL (504.39 mM; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	5.0439 mL	25.2194 mL	50.4388 mL
5 mM	1.0088 mL	5.0439 mL	10.0878 mL
10 mM	0.5044 mL	2.5219 mL	5.0439 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 (12.61 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 (12.61 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 (12.61 mM); 悬浊液; 超声助溶

此方案可获得 2.5 mg/mL的均匀悬浊液，悬浊液可用于口服和腹腔注射。
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 (636 KB) SDS (480 KB)

COA (288 KB) HNMR (224 KB) LCMS (92 KB)

产品使用指南 (1538 KB)

参考文献

[1]. C Scali, et al. Tacrine administration enhances extracellular acetylcholine in vivo and restores the cognitive impairment in aged rats. Pharmacol Res. 1997 Dec;36(6):463-9. [Content Brief]

[2]. Patocka J, et al. Possible role of hydroxylated metabolites of tacrine in drug toxicity and therapy of Alzheimer's disease. Curr Drug Metab. 2008;9(4):332-335. [Content Brief]

[3]. Bhatt S, et al. Assessment of the CYP1A2 Inhibition-Mediated Drug Interaction Potential for Pinocembrin Using In Silico, In Vitro, and In Vivo Approaches. ACS Omega. 2022;7(23):20321-20331. Published 2022 Jun 2. [Content Brief]

[4]. Romero A, et al. Novel tacrine-related drugs as potential candidates for the treatment of Alzheimer's disease. Bioorg Med Chem Lett. 2013;23(7):1916-1922. [Content Brief]

Tacrine 相关分类

Neurological Disease

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	5.0439 mL	25.2194 mL	50.4388 mL	126.0970 mL
	5 mM	1.0088 mL	5.0439 mL	10.0878 mL	25.2194 mL
	10 mM	0.5044 mL	2.5219 mL	5.0439 mL	12.6097 mL
	15 mM	0.3363 mL	1.6813 mL	3.3626 mL	8.4065 mL
	20 mM	0.2522 mL	1.2610 mL	2.5219 mL	6.3049 mL
	25 mM	0.2018 mL	1.0088 mL	2.0176 mL	5.0439 mL
	30 mM	0.1681 mL	0.8406 mL	1.6813 mL	4.2032 mL
	40 mM	0.1261 mL	0.6305 mL	1.2610 mL	3.1524 mL
	50 mM	0.1009 mL	0.5044 mL	1.0088 mL	2.5219 mL
	60 mM	0.0841 mL	0.4203 mL	0.8406 mL	2.1016 mL
	80 mM	0.0630 mL	0.3152 mL	0.6305 mL	1.5762 mL
	100 mM	0.0504 mL	0.2522 mL	0.5044 mL	1.2610 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:

Tacrine321-64-2Cholinesterase (ChE)Alzheimer's diseasehepatotoxicityInhibitorinhibitorinhibit

产品名称：			* 需求量：
* 客户姓名：			* Email：
* 电话：			* 公司或机构名称：
留言给我们：

产品名称：			* Lot #：
* 客户姓名：			* Email：
电话：			* 部门：
* 公司或机构名称：
留言给我们：

MedChemExpress (MCE) 只为有资质的科研机构、医药企业基于科学研究或药证申报的用途提供医药研发服务，不为任何个人或者非科研性质的、非用于药证申报使用等其他用途提供服务。	站点地图隐私声明
沪ICP备15051369号-4 上海工商沪公网安备31011502019417 沪(浦)应急管危经许[2021]201709(QFYS) 营业执照（三证合一）
Copyright © 2013-2025 MedChemExpress. All Rights Reserved.

Tacrine

Customer Review

Other Forms of Tacrine:

MCE 顾客使用本产品发表的 5 篇科研文献

Tacrine 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

稀释计算器

Tacrine 相关分类

完整储备液配制表

Keywords:

您最近查看的产品:

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

姓名
邮箱 *

Sorry, but the email address you supplied was invalid.

Tacrine

Customer Review

Other Forms of Tacrine:

Tacrine 相关抗体

MCE 顾客使用本产品发表的 5 篇科研文献

Tacrine 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

稀释计算器

Tacrine 相关分类

完整储备液配制表

Keywords:

您最近查看的产品:

Request for HNMR Report

Request for HNMR Report

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z