1-[(4-氯苯基)甲基]-2-(吡咯烷-1-基甲基)苯并咪唑
Clemizole
CAS: 442-52-4
Molecular Formula: C19H20ClN3
1-[(4-氯苯基)甲基]-2-(吡咯烷-1-基甲基)苯并咪唑 - Names and Identifiers
1-[(4-氯苯基)甲基]-2-(吡咯烷-1-基甲基)苯并咪唑 - Physico-chemical Properties
| Molecular Formula | C19H20ClN3 |
| Molar Mass | 325.84 |
| Melting Point | 239-241℃ |
| Storage Condition | -20℃ |
| In vitro study | Clemizole hydrochloride is found to inhibit HCV RNA replication in cell culture that is mediated by its suppression of NS4B’s RNA binding, with little toxicity for the host cell. The EC 50 of Clemizole on the W55R mutant J6/JFH RNA is ~18 µM (2.25 times the EC 50 of the wild-type RNA). Clemizole is a novel inhibitor of TRPC5 channels. Clemizole efficiently blocks TRPC5 currents and Ca 2+ entry in the low micromolar range (IC 50 =1.0-1.3 µM). Clemizole exhibits a six-fold selectivity for TRPC5 over TRPC4β (IC 50 =6.4 µM), the closest structural relative of TRPC5, and an almost 10-fold selectivity over TRPC3 (IC 50 =9.1 µM) and TRPC6 (IC 50 =11.3 µM). Clemizole hydrochloride as a novel blocker of TRPC5 with a half-maximal inhibitory concentration of 1.1 µM. The concentration-response curves confirmed a concentration-dependent block of TRPC5 by Clemizole and revealed an apparent IC 50 of 1.1±0.04 µM. |
| In vivo study | Clemizole hydrochloride has an unexpectedly short plasma half-life (measured at 0.15 hours); it is very rapidly biotransformed into a glucuronide (M14) and a dealkylated metabolite (M12) and into a variety of lesser metabolites in C57BL/6J mice. |
1-[(4-氯苯基)甲基]-2-(吡咯烷-1-基甲基)苯并咪唑 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 3.069 ml | 15.345 ml | 30.69 ml |
| 5 mM | 0.614 ml | 3.069 ml | 6.138 ml |
| 10 mM | 0.307 ml | 1.534 ml | 3.069 ml |
| 5 mM | 0.061 ml | 0.307 ml | 0.614 ml |
Last Update：2024-01-02 23:10:35
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