中文名 | 盐酸氯咪唑 |
英文名 | clemizole hydrochloride |
别名 | 盐酸氯咪唑 盐酸克立咪唑 克立咪唑盐酸 克立咪唑盐酸盐 1-对氯苄基-2-(1-吡咯烷基)甲基苯并咪唑 盐酸盐 1-[(4-氯苯基)甲基]-2-(吡咯烷-1-基甲基)苯并咪唑盐酸盐 |
英文别名 | p48 CS-1763 allercur allercurehydrochloride clemizole hydrochloride Clemizole hydrochloride 1-P-CHLOROBENZYL-2-[1-PYRROLIDINYL]-METHYLBENZIMIDAZOLE HYDROCHLORIDE 1-{[1-(4-chlorobenzyl)-1H-benzimidazol-2-yl]methyl}pyrrolidinium chloride 1-[(4-chlorophenyl)methyl]-2-(pyrrolidin-1-ylmethyl)benzimidazole,hydrochloride 1-[(4-Chlorophenyl)methyl]-2-(pyrrolidin-1-ylmethyl)benzoimidazole hydrochloride 1-[(4-Chlorophenyl)methyl]-2-(1-pyrrolidinylmethyl)-1H-benzimidazole hydrochloride 1-[4-Chlorophenyl)methyl]-2-(1-pyrrolidinylmethyl)-1H-benzimidazole, Monohydrochloride |
CAS | 1163-36-6 |
EINECS | 214-605-4 |
化学式 | C19H21Cl2N3 |
分子量 | 362.3 |
InChI | InChI=1/C19H20ClN3.ClH/c20-16-9-7-15(8-10-16)13-23-18-6-2-1-5-17(18)21-19(23)14-22-11-3-4-12-22;/h1-2,5-10H,3-4,11-14H2;1H |
InChIKey | DNFMJYXRIMLMBZ-UHFFFAOYSA-N |
熔点 | 239-241° |
沸点 | 506.1°C at 760 mmHg |
闪点 | 259.9°C |
蒸汽压 | 2.29E-10mmHg at 25°C |
溶解度 | H2O: 可溶物2mg/mL,澄清 (温热) |
存储条件 | Inert atmosphere,2-8°C |
外观 | 粉末 |
颜色 | white to beige |
Merck | 14,2346 |
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. |
危险品标志 | Xn - 有害物品 |
风险术语 | 22 - 吞食有害。 |
安全术语 | 36 - 穿戴适当的防护服。 |
WGK Germany | 3 |
RTECS | DD6730000 |
上游原料 | 邻氯苯甲胺 四氢吡咯 氯化钠 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.76 ml | 13.801 ml | 27.602 ml |
5 mM | 0.552 ml | 2.76 ml | 5.52 ml |
10 mM | 0.276 ml | 1.38 ml | 2.76 ml |
5 mM | 0.055 ml | 0.276 ml | 0.552 ml |
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