1. Neuronal Signaling
  2. Cholinesterase (ChE)
  3. Benactyzine hydrochloride

Benactyzine hydrochloride is a butyrylcholinesterase (BChE) inhibitor with a Ki of 0.010 mM.

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

Benactyzine hydrochloride Chemical Structure

Benactyzine hydrochloride Chemical Structure

CAS No. : 57-37-4

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Solid + Solvent
10 mM * 1 mL in DMSO
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Based on 1 publication(s) in Google Scholar

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Description

Benactyzine hydrochloride is a butyrylcholinesterase (BChE) inhibitor with a Ki of 0.010 mM.

IC50 & Target

Ki: 0.010 mM (BChE)[1]

In Vitro

Benactyzine hydrochloride and drofenine are widely used anticholinergic drugs which are also competitive inhibitors of BChE with Ki values of 0.010±0.001 and 0.003±0.000 mM, respectively. Results indicate that the inhibition of BChE by Benactyzine hydrochloride is pure or partial competitive. Pure competitive inhibition can be distinguished from partial competitive inhibition by plotting v vs [Benactyzine] at a fixed [BTCh][1].

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

In Vivo

Benactyzine hydrochloride (1 mg/kg) does not influence the attention response. Benactyzine hydrochloride increases the duration of the exploratory-motor reaction, but slightly diminishes the salivation elicited by acetylcholine. There is no blocking effect of Benactyzine hydrochloride and promazine on the EEG-seizure activity elicited by acetylcholine, and almost no inhibitory effect on emotional reactions. Emotional reactions are blocked by high doses of imipramine and promazine, but not by Benactyzine hydrochloride. The data indicates that imipramine, promazine and Benactyzine hydrochloride influence the autonomic effects of serotonin in different ways. Promazine, and especially Benactyzine hydrochloride, inhibit and shorten the period of salivation elicited by the intra-amygdaloid injection of serotonin[2].

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

Molecular Weight

363.88

Formula

C20H26ClNO3

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(OCCN(CC)CC)C(C1=CC=CC=C1)(O)C2=CC=CC=C2.[H]Cl

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: 

DMSO : 150 mg/mL (412.22 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 50 mg/mL (137.41 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7482 mL 13.7408 mL 27.4816 mL
5 mM 0.5496 mL 2.7482 mL 5.4963 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). 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

=
Concentration (final)

C2

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Volume (final)

V2

In Vivo:

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: 25 mg/mL (68.70 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

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
References
Kinase Assay
[1]

Butyrylcholinesterase activity is measured spectrophotometrically with spectrophotometer using butyrylthiocholine iodide (BTCh) as substrate. In the kinetic studies, initial velocities are measured at 37°C by using 0.25 mM 5,5’-dithio-bis(2-nitrobenzoic acid) (DTNB) in 5 mM 3-(N-morpholino)propanesulfonic acid (MOPS) buffer, pH 7.5, and appropriate concentrations of Benactyzine hydrochloride and drofenine solutions prepared in water, as a function of BTCh concentration from 0.25 to 5.0 mM BTCh in 0.5 mL final volume of assay mixture (0.5 mL assay mixture contains 1.56 mg purified enzyme). Assays are carried out in duplicate and activities are measured for up to 90 s[1].

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

Animal Administration
[2]

Experiments are carried out in 36 cats of both sexes weighing 1.8 to 4 kg in a free-behavior situation. The experiments are carried out in the following order: after the first micro-injection of acetylcholine and/or serotonin and/or noradrenaline (200 μg) into the amygdala the changes in the behavior, autonomic reactions and EEG are recorded for a period of 10 min and then followed by intramuscular injections of imipramine and/or Benactyzine hydrochloride and/or promazine and/or saline (in control experiments). The second micro-injection of neurohormones (200 μg) into the amygdala is performed in 45 rain after the intramuscular injection of drugs and/or saline, and the effect is compared with the previous one, induced by the first micro-injection[2].

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

References

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). 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 / DMSO 1 mM 2.7482 mL 13.7408 mL 27.4816 mL 68.7040 mL
5 mM 0.5496 mL 2.7482 mL 5.4963 mL 13.7408 mL
10 mM 0.2748 mL 1.3741 mL 2.7482 mL 6.8704 mL
15 mM 0.1832 mL 0.9161 mL 1.8321 mL 4.5803 mL
20 mM 0.1374 mL 0.6870 mL 1.3741 mL 3.4352 mL
25 mM 0.1099 mL 0.5496 mL 1.0993 mL 2.7482 mL
30 mM 0.0916 mL 0.4580 mL 0.9161 mL 2.2901 mL
40 mM 0.0687 mL 0.3435 mL 0.6870 mL 1.7176 mL
50 mM 0.0550 mL 0.2748 mL 0.5496 mL 1.3741 mL
60 mM 0.0458 mL 0.2290 mL 0.4580 mL 1.1451 mL
80 mM 0.0344 mL 0.1718 mL 0.3435 mL 0.8588 mL
100 mM 0.0275 mL 0.1374 mL 0.2748 mL 0.6870 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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