Tacrine hydrochloride (hydrate)

Name: Tacrine hydrochloride (hydrate)
Brand: MedChemExpress
SKU: HY-B2244
Rating: 5.0 (5 reviews)

Cat. No.: HY-B2244 Purity: 99.98%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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.

Tacrine hydrochloride (hydrate) Chemical Structure

CAS No. : 206658-92-6

Size	Price	Stock	Quantity
Solution
10 mM * 1 mL in DMSO	USD 39	In-stock	Estimated Time of Arrival: December 31
Solid
100 mg	USD 35	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 5 publication(s) in Google Scholar

Other Forms of Tacrine hydrochloride (hydrate):

Tacrine hydrochloride In-stock

5 Publications Citing Use of MCE Tacrine hydrochloride (hydrate)

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Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

Tacrine hydrochloride (hydrate) is an inhibitor of both acetyl (AChE) and butyryl-cholinestrase (BChE) with IC₅₀s of 31 nM and 25.6 nM, respectively.

IC₅₀ & Target

IC50: 31 nM (AChE), 25.6 nM (BChE)

In Vitro

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.

In Vivo

Pretreatment with Tacrine hydrochloride (hydrate) also modifies absolute levels of cocaine self-administration during reacquisition. Body weight declines approximately one-half percent over four days of treatment with intravenous Tacrine hydrochloride (hydrate). Delivery of Tacrine hydrochloride (hydrate) by osmotic pump does not alter either linear- or repeated- cocaine-induced locomotor activity. There is no significant main effect or interaction with Tacrine hydrochloride (hydrate) treatment on active lever responding during reinstatement. Post hoc comparisons indicate that rats self-administering cocaine has significantly lower alkaline phosphatase levels, relative to TTacrine hydrochloride (hydrate)- but not saline- treated rats evaluated by conditioned-place preference^[2].

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

Clinical Trial

Formula

C₁₃H₁₄N₂.xHCl.xH₂O

CAS No.

206658-92-6

Appearance

Solid

Color

White to off-white

SMILES

NC1=C(CCCC2)C2=NC3=CC=CC=C31.[H]Cl.[H]O[H].[x].[x]

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

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

Solvent & Solubility

In Vitro:

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)

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

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 (Infinity 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 (Infinity 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 (Infinity mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.

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.

Protocol 1

Add each solvent one by one: PBS
Solubility: 100 mg/mL (Infinity mM); Clear solution; Need ultrasonic

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.

Calculation results:

Working solution concentration: mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

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).

Purity & Documentation

Purity: 99.98%

Select Batch:

Data Sheet (278 KB) SDS (584 KB)

COA (251 KB) HNMR (190 KB) LCMS (405 KB)

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]

Kinase Assay ^[1]	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]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[2]	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]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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]