1. Neuronal Signaling
  2. AChE
  3. Tacrine hydrochloride hydrate

Tacrine hydrochloride hydrate 

Cat. No.: HY-B2244 Purity: 99.98%
Handling Instructions

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

Tacrine hydrochloride hydrate Chemical Structure

CAS No. : 206658-92-6

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 66 In-stock
Estimated Time of Arrival: December 31
100 mg USD 60 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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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].

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 Tacrine hydrochloride hydrate- but not saline- treated rats evaluated by conditioned-place preference[2].

Clinical Trial
Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 32 mg/mL (126.61 mM; Need ultrasonic and warming)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.9566 mL 19.7832 mL 39.5664 mL
5 mM 0.7913 mL 3.9566 mL 7.9133 mL
10 mM 0.3957 mL 1.9783 mL 3.9566 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (9.89 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (9.89 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (9.89 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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
Molecular Weight

252.74

Formula

C₁₃H₁₇ClN₂O

CAS No.

206658-92-6

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
Tacrine hydrochloride hydrate
Cat. No.:
HY-B2244
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Tacrine hydrochloride hydrate

Cat. No.: HY-B2244