1. Telenzepine dihydrochloride

Telenzepine dihydrochloride is a selective and orally active muscarinic M1 receptor antagonist with a Ki of 0.94 nM. Telenzepine dihydrochloride inhibits gastric acid secretion and has antiulcer effects.

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

Telenzepine dihydrochloride Chemical Structure

Telenzepine dihydrochloride Chemical Structure

CAS No. : 147416-96-4

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5 mg USD 95 In-stock
10 mg USD 150 In-stock
25 mg USD 280 In-stock
50 mg USD 450 In-stock
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Description

Telenzepine dihydrochloride is a selective and orally active muscarinic M1 receptor antagonist with a Ki of 0.94 nM. Telenzepine dihydrochloride inhibits gastric acid secretion and has antiulcer effects[1][2][3].

IC50 & Target

Ki: 0.94 nM (Muscarinic M1 receptor), 17.8 nM (Muscarinic M2 receptor)[3]

In Vitro

At submicromolar concentrations (100 nM), Telenzepine abolishes responses to either muscarine or the muscarinic component of the acetylcholine response. The excitatory effect of muscarine at postsynaptic M1 receptors is dose dependently inhibited by Telenzepine (0.1-1000 nM) at concentrations[2].
The threshold dose of Telenzepine as an antagonist of the muscarinic depolarization in AH/type 2 neurons is in the range of 0.1-1 nM. The IC50 of Telenzepine needed to abolish the response is 8.5 nM[2].

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

In Vivo

Intravenous Telenzepine potently inhibits gastric acid secretion in the Ghosh-Schild rat (carbachol-stimulated), the chronic fistula rat (basal secretion), or, both intravenously and orally, in the modified Shay rat[1].
Telenzepine (2.7 μmol/kg; orally) treatment shows significantly longer duration antiulcer effects in the modified Shay rat[1].

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

Clinical Trial
Molecular Weight

443.39

Formula

C19H24Cl2N4O2S

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C1C2=CSC(C)=C2N(C(CN3CCN(C)CC3)=O)C4=CC=CC=C4N1.[H]Cl.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°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 : 62.5 mg/mL (140.96 mM; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2554 mL 11.2768 mL 22.5535 mL
5 mM 0.4511 mL 2.2554 mL 4.5107 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)

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

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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.
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

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 1 mM 2.2554 mL 11.2768 mL 22.5535 mL 56.3838 mL
5 mM 0.4511 mL 2.2554 mL 4.5107 mL 11.2768 mL
10 mM 0.2255 mL 1.1277 mL 2.2554 mL 5.6384 mL
15 mM 0.1504 mL 0.7518 mL 1.5036 mL 3.7589 mL
20 mM 0.1128 mL 0.5638 mL 1.1277 mL 2.8192 mL
25 mM 0.0902 mL 0.4511 mL 0.9021 mL 2.2554 mL
30 mM 0.0752 mL 0.3759 mL 0.7518 mL 1.8795 mL
40 mM 0.0564 mL 0.2819 mL 0.5638 mL 1.4096 mL
50 mM 0.0451 mL 0.2255 mL 0.4511 mL 1.1277 mL
60 mM 0.0376 mL 0.1879 mL 0.3759 mL 0.9397 mL
80 mM 0.0282 mL 0.1410 mL 0.2819 mL 0.7048 mL
100 mM 0.0226 mL 0.1128 mL 0.2255 mL 0.5638 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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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
Telenzepine dihydrochloride
Cat. No.:
HY-B1789A
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