Telenzepine dihydrochloride
Based on 1 Customer Validation
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.
- Purity: 99.57%
- CAS No.: 147416-96-4
- Formula: C19H24Cl2N4O2S
- Molecular Weight:443.39
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Storage:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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mAChR1 |
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.
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.
Chemical Information
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CAS No. 147416-96-4
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Appearance Solid
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Molecular Weight 443.39
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Formula C19H24Cl2N4O2S
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Color White to off-white
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SMILES
O=C1C2=CSC(C)=C2N(C(CN3CCN(C)CC3)=O)C4=CC=CC=C4N1.[H]Cl.[H]Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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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
H2O : 62.5 mg/mL (140.96 mM; ultrasonic and warming and heat to 60°C)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (277 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. R Riedel, et al. Comparison of the gastric antisecretory and antiulcer potencies of telenzepine, pirenzepine, ranitidine and cimetidine in the rat. Digestion. 1988;40(1):25-32. [Content Brief]
[2]. F L Christofi, et al. Neuropharmacology of the muscarinic antagonist telenzepine in myenteric ganglia of the guinea-pig small intestine. Eur J Pharmacol. 1991 Apr 3;195(3):333-9. [Content Brief]
[3]. M Galvan, et al. Interaction of telenzepine with muscarinic receptors in mammalian sympathetic ganglia. Eur J Pharmacol. 1989 Aug 11;167(1):1-10. [Content Brief]
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.
Telenzepine dihydrochloride Related Classifications
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