Tacrine

目錄號(hào): HY-111338 純度: 99.91%: FAQs
Data Sheet SDS COA 產(chǎn)品使用指南

摩爾計(jì)算器

Tacrine 是一種可口服的有效的乙酰膽堿 (AChE) 抑制劑 (IC₅₀=109 nM)，同時(shí)也是一種 CYP1A2 底物活性分子。Tacrine 可恢復(fù)老年大鼠的認(rèn)知功能障礙。Tacrine 可沉淀肝毒性并用于阿爾茲海默癥的研究。

MCE 的所有產(chǎn)品僅用作科學(xué)研究或藥證申報(bào)，我們不為任何個(gè)人用途提供產(chǎn)品和服務(wù)

Tacrine Chemical Structure

CAS No. : 321-64-2

1. 客戶無需承擔(dān)相應(yīng)的運(yùn)輸費(fèi)用。

2. 同一機(jī)構(gòu)（單位）同一產(chǎn)品試用裝僅限申領(lǐng)一次，同一機(jī)構(gòu)（單位）一年內(nèi)

可免費(fèi)申領(lǐng)三個(gè)不同產(chǎn)品的試用裝。

3. 試用裝只面向終端客戶。

規(guī)格	價(jià)格	是否有貨
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	現(xiàn)貨	詢價(jià)
1 g		詢價(jià)
5 g		詢價(jià)

or 大包裝詢價(jià)

* Please select Quantity before adding items.

Customer Review

Other Forms of Tacrine:

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

MCE 顧客使用本產(chǎn)品發(fā)表的 5 篇科研文獻(xiàn)

•Cell Death Dis. 2022 Jan 10;13(1):48. [Abstract]
•Eur J Med Chem. 2023 Dec 21, 116071.
•Bioorg Chem. 2023 Nov 29, 107010.
•J Enzyme Inhib Med Chem. 2023 Dec;38(1):2192439. [Abstract]
•Front Neurosci. 2020 May 28:14:458. [Abstract]

Tacrine 相關(guān)產(chǎn)品

•相關(guān)化合物庫(kù):

•同靶點(diǎn)產(chǎn)品:

•同靶點(diǎn)蛋白產(chǎn)品:

查看 Cholinesterase (ChE) 亞型特異性產(chǎn)品:

查看所有亞型

AChE BChE

生物活性
純度 & 產(chǎn)品資料
參考文獻(xiàn)

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)

細(xì)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]

體內(nèi)研究
(In Vivo)

Tacrine (0.3-3 mg/kg，口服，單次劑量) 增加大鼠海馬細(xì)胞外乙酰膽堿水平，改善行為功能^[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 號(hào)

321-64-2

性狀

固體

顏色

Off-white to light yellow

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.

儲(chǔ)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)

溶解性數(shù)據(jù)

細(xì)胞實(shí)驗(yàn)：

DMSO 中的溶解度 : ≥ 100 mg/mL (504.39 mM; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響，請(qǐng)使用新開封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制儲(chǔ)備液

濃度溶劑體積質(zhì)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

查看完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備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儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用。

摩爾計(jì)算器
稀釋計(jì)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

濃度 _(start)

體積 _(start)

濃度 _(final)

體積 _(final)

動(dòng)物實(shí)驗(yàn)：

請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥方式選擇適當(dāng)?shù)娜芙夥桨浮?

以下溶解方案都請(qǐng)先按照 In Vitro 方式配制澄清的儲(chǔ)備液，再依次添加助溶劑：
——為保證實(shí)驗(yàn)結(jié)果的可靠性，澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用；
以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶

方案一

請(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (12.61 mM); 澄清溶液

此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液。
以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 400 μL PEG300 中，混合均勻；再向上述體系中加入 50 μL Tween-80，混合均勻；然后再繼續(xù)加入 450 μL 生理鹽水定容至 1 mL。
生理鹽水的配制：將 0.9 g 氯化鈉，溶解于 ddH?O 并定容至 100 mL，可以得到澄清透明的生理鹽水溶液。
方案二

請(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (12.61 mM); 澄清溶液

此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液。
以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液中，混合均勻。
2 g SBE-β-CD（磺丁基醚 β-環(huán)糊精）粉末定容于 10 mL 的生理鹽水中，完全溶解至澄清透明。
方案三

請(qǐng)依序添加每種溶劑： 10% DMSO 90% Corn Oil
Solubility: 2.5 mg/mL (12.61 mM); 懸濁液; 超聲助溶

此方案可獲得 2.5 mg/mL的均勻懸濁液，懸濁液可用于口服和腹腔注射。
以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 900 μL玉米油中，混合均勻。

動(dòng)物溶解方案計(jì)算器

請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息：

給藥劑量

mg/kg

動(dòng)物的平均體重

每只動(dòng)物的給藥體積

μL

動(dòng)物數(shù)量

只

由于實(shí)驗(yàn)過程有損耗，建議您多配一只動(dòng)物的量

請(qǐng)輸入您的動(dòng)物體內(nèi)配方組成：

DMSO +

Tween-80 +

Saline

如果您的動(dòng)物是免疫缺陷鼠或者體弱鼠，建議 DMSO 中的在最后工作液體系中的占比盡量不超過 2%。

方案所需 助溶劑 包括：DMSO，，均可在 MCE 網(wǎng)站選購(gòu)。，Tween 80，均可在 MCE 網(wǎng)站選購(gòu)。

計(jì)算結(jié)果

工作液所需濃度 : mg/mL

儲(chǔ)備液配制方法 : mg 藥物溶于 μL DMSO（母液濃度為 mg/mL）。

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

您所需的儲(chǔ)備液濃度超過該產(chǎn)品的實(shí)測(cè)溶解度，以下方案僅供參考，如有需要，請(qǐng)與 MCE 中國(guó)技術(shù)支持聯(lián)系。

動(dòng)物實(shí)驗(yàn)體內(nèi)工作液的配制方法 : 取 μL DMSO 儲(chǔ)備液，加入 μL 。 μL ，混合均勻至澄清，再加 μL Tween 80，混合均勻至澄清，再加 μL 生理鹽水。

連續(xù)給藥周期超過半月以上，請(qǐng)謹(jǐn)慎選擇該方案。

請(qǐng)確保第一步儲(chǔ)備液溶解至澄清狀態(tài)，從左到右依次添加助溶劑。您可采用超聲加熱（超聲清洗儀，建議頻次 20-40 kHz），渦旋吹打等方式輔助溶解。

純度 & 產(chǎn)品資料

純度: 99.91%

選擇批次：

Data Sheet (636 KB) SDS (480 KB)

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

產(chǎn)品使用指南 (1538 KB)

參考文獻(xiàn)

[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 相關(guān)分類

Neurological Disease

完整儲(chǔ)備液配制表

可選溶劑	濃度溶劑體積質(zhì)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

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Tacrine

Customer Review

Other Forms of Tacrine:

MCE 顧客使用本產(chǎn)品發(fā)表的 5 篇科研文獻(xiàn)

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Tacrine

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Other Forms of Tacrine:

Tacrine 相關(guān)抗體

MCE 顧客使用本產(chǎn)品發(fā)表的 5 篇科研文獻(xiàn)

Tacrine 相關(guān)產(chǎn)品

•相關(guān)化合物庫(kù):

•同靶點(diǎn)產(chǎn)品:

•同靶點(diǎn)蛋白產(chǎn)品:

查看 Cholinesterase (ChE) 亞型特異性產(chǎn)品:

生物活性

純度 & 產(chǎn)品資料

參考文獻(xiàn)

摩爾計(jì)算器

稀釋計(jì)算器

Tacrine 相關(guān)分類

完整儲(chǔ)備液配制表

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