Tacrine

Name: Tacrine
Brand: MedChemExpress
SKU: HY-111338
Rating: 5.0 (5 reviews)

Cat. No.: HY-111338 Purity: 99.91%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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.

For research use only. We do not sell to patients.

Tacrine Chemical Structure

CAS No. : 321-64-2

Size	Price	Stock	Quantity
5 mg	USD 80	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 120	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 280	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 450	In-stock	Estimated Time of Arrival: December 31
500 mg	USD 860	In-stock	Estimated Time of Arrival: December 31
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5 g		Get quote

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Customer Review

Based on 5 publication(s) in Google Scholar

Other Forms of Tacrine:

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

5 Publications Citing Use of MCE Tacrine

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AChE BChE

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

AChE

109 nM (IC₅₀)

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]

In Vivo

Tacrine (0.3-3 mg/kg, orally, single dose) increases extracellular acetylcholine levels in rat hippocampus and improves behavioral function^[1].

MedChemExpress (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

Molecular Weight

198.26

Formula

C₁₃H₁₄N₂

CAS No.

321-64-2

Appearance

Solid

Color

Off-white to light yellow

SMILES

NC1=C2CCCCC2=NC3=CC=CC=C31

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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)

Solvent & Solubility

In Vitro:

DMSO : ≥ 100 mg/mL (504.39 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

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

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (12.61 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (12.61 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: 2.5 mg/mL (12.61 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

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

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.91%

Select Batch:

Data Sheet (301 KB) SDS (480 KB)

COA (251 KB) HNMR (224 KB) LCMS (92 KB)

Handling Instructions (2659 KB)

References

[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]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	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

Tacrine Related Classifications

Neurological Disease

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

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5 Publications Citing Use of MCE Tacrine

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View All Cholinesterase (ChE) Isoform Specific Products:

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Purity & Documentation

References

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Complete Stock Solution Preparation Table

Tacrine Related Classifications

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