Tacrine hydrochloride
Based on 8 publication(s) in Google Scholar
Tacrine hydrochloride is a potent brain-penetrant inhibitor of both AChE and BChE, with IC50s of 31 nM and 25.6 nM, respectively. Tacrine hydrochloride is also a NMDAR inhibitor, with an IC50 of 26 μM. Tacrine hydrochloride can be used for the research of Alzheimer’s disease.
For research use only. We do not sell to patients.
- Purity: 99.90%
- CAS No.: 1684-40-8
- Formula: C13H15ClN2
- Molecular Weight:234.73
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Storage:
4°C, stored under nitrogen, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Tacrine hydrochloride
More- Cell Death Dis. 2022 Jan 10;13(1):48. [Abstract]
- Drug Deliv. 2025 Dec 31;32(1):2585612. [Abstract]
- J Med Chem. 2025 Nov 27;68(22):24326-24357. [Abstract]
- Eur J Med Chem. 2024 Feb 5:265:116071. [Abstract]
- J Enzyme Inhib Med Chem. 2023 Dec;38(1):2192439. [Abstract]
- Bioorg Chem. 2024 Feb:143:107010. [Abstract]
- J Neurochem. 2025 Aug;169(8):e70178. [Abstract]
- Front Neurosci. 2020 May 28:14:458. [Abstract]
All iGluR Isoforms
More
Biological Activity
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AChE |
BChE |
NMDA Receptor |
Tacrine (12.5-37.5 nM) inhibits venom acetylcholinesterase as well as human serum butyrylcholinesterase in a concentration-dependent manner[1].
Tacrine reduces the neurotoxicity induced by the activation of the NMDARs in murine cortical neuronal cultures with an IC50of ~500 μM[2].
Tacrine inhibits the NMDAR responses in a concentration-dependent manner with an IC50 of ~190 μM at -60 mV[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Tacrine (0.1-0.4 mg/mL; i.p. for 7 d) inhibits the expression of AChE, but does not significantly improve the protection of the retina function and morphology in mice[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1684-40-8
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Appearance Solid
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Molecular Weight 234.73
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Formula C13H15ClN2
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Color White to light yellow
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SMILES
NC1=C(CCCC2)C2=NC3=CC=CC=C31.[H]Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, stored under nitrogen, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)
Publications (8)
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Journal Impact Factor
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Most Recent
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Cell Death Dis
A fragment of cell adhesion molecule L1 reduces amyloid-β plaques in a mouse model of Alzheimer's disease. [Abstract]2022 Jan 10;13(1):48. PMID: 35013124 -
Drug Deliv
A surrogate barrier model for high-throughput blood-brain barrier permeability prediction: integrating LLC-PK1-MOCK/MDR1 Cells and lysosomal trapping correction. [Abstract]2025 Dec 31;32(1):2585612. PMID: 41307200 -
J Med Chem
Fluorocyclopropyl-Containing Tacrine Derivatives as Potent and Selective Dual CDK2/CDK9 Inhibitors for the Treatment of Colorectal Cancer. [Abstract]2025 Nov 27;68(22):24326-24357. PMID: 41239996 -
Eur J Med Chem
Design, synthesis and biological evaluation of carbamate derivatives incorporating multifunctional carrier scaffolds as pseudo-irreversible cholinesterase inhibitors for the treatment of Alzheimer's disease. [Abstract]2024 Feb 5:265:116071. PMID: 38157596 -
J Enzyme Inhib Med Chem
Design, synthesis and evaluation of OA-tacrine hybrids as cholinesterase inhibitors with low neurotoxicity and hepatotoxicity against Alzheimer's disease. [Abstract]2023 Dec;38(1):2192439. PMID: 36950955 -
Bioorg Chem
Design, synthesis, and biological evaluation of novel donepezil-tacrine hybrids as multi-functional agents with low neurotoxicity against Alzheimer's disease. [Abstract]2024 Feb:143:107010. PMID: 38056387 -
J Neurochem
The Tacrine-Induced Endoplasmic Reticulum Stress in AChE-Expressed Cells Leads to Improper Assembly and Transport of the Oligomeric Enzyme: Reversal by Trehalose. [Abstract]2025 Aug;169(8):e70178. PMID: 40762084 -
Front Neurosci
Adhesion Molecule L1 Agonist Mimetics Protect Against the Pesticide Paraquat-Induced Locomotor Deficits and Biochemical Alterations in Zebrafish. [Abstract]2020 May 28:14:458. PMID: 32547358
Solvent & Solubility
H2O : 33.33 mg/mL (141.99 mM; Need ultrasonic)
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 (stored under nitrogen, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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 (stored under nitrogen, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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.
Add each solvent one by one: PBS
Solubility: 16.67 mg/mL (71.02 mM); Clear solution; Need ultrasonic
Purity & Documentation
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Data Sheet (274 KB)
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SDS (644 KB)
- English - EN (644 KB)
- Français - FR (644 KB)
- Deutsch - DE (644 KB)
- Norwegian - NO (644 KB)
- Español - ES (644 KB)
- Swedish - SV (644 KB)
- Italian - IT (644 KB)
- Portuguese - PT (644 KB)
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Handling Instructions (2659 KB)
References
[1]. Ahmed M, et, al. Inhibition of two different cholinesterases by tacrine. Chem Biol Interact. 2006 Aug 25; 162(2):165-71.c [Content Brief]
[2]. Horak M, et, al. The pharmacology of tacrine at N-methyl-d-aspartate receptors. Prog Neuropsychopharmacol Biol Psychiatry. 2017 Apr 3;75: 54-62. [Content Brief]
[3]. The protective role of tacrine and donepezil in the retina of acetylcholinesterase knockout mice. Yi YM, et, al. Int J Ophthalmol. 2015 Oct 18; 8(5): 884-90. [Content Brief]
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 (stored under nitrogen, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O | 1 mM | 4.2602 mL | 21.3011 mL | 42.6021 mL | 106.5053 mL |
| 5 mM | 0.8520 mL | 4.2602 mL | 8.5204 mL | 21.3011 mL | |
| 10 mM | 0.4260 mL | 2.1301 mL | 4.2602 mL | 10.6505 mL | |
| 15 mM | 0.2840 mL | 1.4201 mL | 2.8401 mL | 7.1004 mL | |
| 20 mM | 0.2130 mL | 1.0651 mL | 2.1301 mL | 5.3253 mL | |
| 25 mM | 0.1704 mL | 0.8520 mL | 1.7041 mL | 4.2602 mL | |
| 30 mM | 0.1420 mL | 0.7100 mL | 1.4201 mL | 3.5502 mL | |
| 40 mM | 0.1065 mL | 0.5325 mL | 1.0651 mL | 2.6626 mL | |
| 50 mM | 0.0852 mL | 0.4260 mL | 0.8520 mL | 2.1301 mL | |
| 60 mM | 0.0710 mL | 0.3550 mL | 0.7100 mL | 1.7751 mL | |
| 80 mM | 0.0533 mL | 0.2663 mL | 0.5325 mL | 1.3313 mL | |
| 100 mM | 0.0426 mL | 0.2130 mL | 0.4260 mL | 1.0651 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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