Tacrine hydrochloride hydrate
Based on 8 publication(s) in Google Scholar
Tacrine hydrochloride (hydrate) is an inhibitor of both acetyl (AChE) and butyryl-cholinestrase (BChE) with IC50s of 31 nM and 25.6 nM, respectively.
For research use only. We do not sell to patients.
- Purity: 99.98%
- CAS No.: 206658-92-6
- Formula: C13H14N2.xHCl.xH2O
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Tacrine hydrochloride hydrate
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]
Biological Activity
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AChE |
BChE |
Tacrine hydrochloride (hydrate) (12.5 to 37.5 nM) inhibits venom acetylcholinesterase as well as human serum butyrylcholinesterase in a concentration-dependent manner. The IC50 is 31 nM for snake venom AChE and 25.6 nM for human BChE[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 206658-92-6
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Appearance Solid
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Formula C13H14N2.xHCl.xH2O
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Color White to off-white
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SMILES
NC1=C(CCCC2)C2=NC3=CC=CC=C31.[H]Cl.[H]O[H].[x].[x]
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, 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 : 100 mg/mL (Need ultrasonic)
DMSO : 32 mg/mL (Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL; 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL; 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.
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: 100 mg/mL; Clear solution; Need ultrasonic
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Protocol
The kinetic parameters of the interaction between Tacrine hydrochloride hydrate and cholinesterase are determined using the double reciprocal plot analyzed over a range of acetylthiocholine concentrations (0.05 to 1 mM) in the absence and in the presence of Tacrine hydrochloride hydrate (12.5 to 37.5 nM). IC50 is determined by percentage residual activity versus concentration of Tacrine hydrochloride hydrate[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Male Wistar rats at 9 weeks of age are used in this study. As soon as rats exhibit a stable pattern of self-administration under fixed-ratio-5 (FR-5) with a 20-second time out, sessions are discontinued over 24 hours and rats are left undisturbed in home cages, attached to a fluid swivel and steel-coil tether. This initial washout interval is assessed as more than adequate to allow clearance of plasma cocaine, which has a half-life of less than 20 minutes in rats. Beginning on the following day, 10 mg/kg-day of Tacrine hydrochloride hydrate or vehicle (saline) is administered as a chronic infusion over 4 days, delivered intravenously at 4.0 ml per day. After completion of these infusions, rats are then left undisturbed in home cages for an additional two days. This second washout period permits complete clearance of Tacrine hydrochloride hydrate, which has a half-life of less than two hours in rat brain. Cocaine self-administration is then re-initiated under FR-5 with a 20-second time-out period. To determine persistent effects of Tacrine hydrochloride hydrate, the pattern of self-administration is monitored over six additional sessions[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (278 KB)
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SDS (420 KB)
- English - EN (420 KB)
- Français - FR (420 KB)
- Deutsch - DE (420 KB)
- Norwegian - NO (420 KB)
- Español - ES (420 KB)
- Swedish - SV (420 KB)
- Italian - IT (420 KB)
- Korean - KR (420 KB)
- Portuguese - PT (420 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. [Content Brief]
[2]. Grasing K, et al. Enduring effects of tacrine on cocaine-reinforced behavior: Analysis by conditioned-place preference, temporal separation from drug reward, and reinstatement. Pharmacol Res. 2015 Jul;97:40-7. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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