1-[(4-氯苯基)甲基]-2-(吡咯烷-1-基甲基)苯并咪唑盐酸盐
中文名称 | 1-[(4-氯苯基)甲基]-2-(吡咯烷-1-基甲基)苯并咪唑盐酸盐 |
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中文同义词 | 1-[(4-氯苯基)甲基]-2-(吡咯烷-1-基甲基)苯并咪唑盐酸盐;1-对氯苄基-2-(1-吡咯烷基)甲基苯并咪唑 盐酸盐;克立咪唑盐酸;盐酸氯咪唑;盐酸克立咪唑, >98%;盐酸克立咪唑;克立咪唑盐酸盐;1-(4-氯苄基)-2-(吡咯烷-1-基甲基)-1H-苯并[D]咪唑盐酸盐 |
英文名称 | Clemizole hydrochloride |
英文同义词 | allercur;allercurehydrochloride;p48;1-P-CHLOROBENZYL-2-[1-PYRROLIDINYL]-METHYLBENZIMIDAZOLE HYDROCHLORIDE;1-[(4-Chlorophenyl)methyl]-2-(pyrrolidin-1-ylmethyl)benzoimidazole hydrochloride;CLEMIZOLE HCL;CLEMIZOLE HYDROCHLORIDE;LABOTEST-BB LT00453174 |
CAS号 | 1163-36-6 |
分子式 | C19H21Cl2N3 |
分子量 | 362.3 |
EINECS号 | 214-605-4 |
相关类别 | 抑制剂;小分子抑制剂;小分子抑制剂,天然产物;Inhibitors |
Mol文件 | 1163-36-6.mol |
结构式 |
1-[(4-氯苯基)甲基]-2-(吡咯烷-1-基甲基)苯并咪唑盐酸盐 性质
熔点 | 239-241° |
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储存条件 | Inert atmosphere,2-8°C |
溶解度 | 在水中的溶解度为性2mg/mL,澄清(加热) |
形态 | 粉末 |
颜色 | 白色至米色 |
水溶解性 | 16.84mg/L at 25℃ |
Merck | 14,2346 |
InChIKey | DNFMJYXRIMLMBZ-UHFFFAOYSA-N |
LogP | 1.99 |
CAS 数据库 | 1163-36-6(CAS DataBase Reference) |
IC50: 24 nM (NS4B)
H1 histamine receptor
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.
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.
提供商 | 语言 |
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英文
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