1-(4-chlorobenzyl)-2-(pyrrolidin-1-ylmethyl)benzimidazole
Clemizole(Clemizole)
CAS: 442-52-4
化学式: C19H20ClN3
| 中文名 | Clemizole |
| 英文名 | Clemizole |
| 别名 | 吡咯咪唑 吡咯咪唑盐酸盐 1-[(4-氯苯基)甲基]-2-(吡咯烷-1-基甲基)苯并咪唑 |
| 英文别名 | Histacur Clemizole Clemizole (free base) 1-(4-Chlorobenzyl)-2-(pyrrolizinomethyl)-1H-benzimidazole 1-(4-chlorobenzyl)-2-(pyrrolidin-1-ylmethyl)benzimidazole 1-(p-Chlorobenzyl)-2-(1-pyrrolidinylmethyl)-1H-benzimidazole 1-[(4-chlorophenyl)methyl]-2-(pyrrolidin-1-ylmethyl)benzimidazole 1-[(4-chlorophenyl)methyl]-2-(1-pyrrolidinylmethyl)-1H-benzimidazole 1-[(4-chlorophenyl)methyl]-2-(1-pyrrolidinylmethyl)-1H-benzimidazole(Clemizole) |
| CAS | 442-52-4 |
| EINECS | 207-133-5 |
| 化学式 | C19H20ClN3 |
| 分子量 | 325.84 |
| 熔点 | 239-241℃ |
| 存储条件 | -20℃ |
| 体外研究 | 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. |
| 体内研究 | 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. |
| 上游原料 | 氢氧化钠 乙酸乙酯 甲醇 二氯甲烷 N,N-二甲基甲酰胺 甲苯 三氯氧磷 亚硝酸钠 氯化亚锡二水合物 对氯苯甲醛 氯乙酰氯 四氢吡咯 对甲苯磺酸水合物 邻氯硝基苯 |
1-(4-chlorobenzyl)-2-(pyrrolidin-1-ylmethyl)benzimidazole - 配置溶液浓度参考
| 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 |
最后更新：2024-01-02 23:10:35
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1-(4-chlorobenzyl)-2-(pyrrolidin-1-ylmethyl)benzimidazole的上游原料
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