吡咯咪唑 CAS#: 442-52-4

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吡咯咪唑

用途生物活性靶点体外研究体内研究 用途与合成方法 MSDS 吡咯咪唑价格(试剂级) 上下游产品信息 专题

中文名称	吡咯咪唑
中文同义词	1-[(4-氯苯基)甲基]-2-(吡咯烷-1-基甲基)苯并咪唑;吡咯咪唑盐酸盐;吡咯咪唑
英文名称	Clemizole
英文同义词	Clemizole (free base);1-[(4-chlorophenyl)methyl]-2-(1-pyrrolidinylmethyl)-1H-benzimidazole (Clemizole);1-(4-Chlorobenzyl)-2-(pyrrolizinomethyl)-1H-benzimidazole;1-(p-Chlorobenzyl)-2-(1-pyrrolidinylmethyl)-1H-benzimidazole;Histacur;1-(4-chlorobenzyl)-2-(pyrrolidin-1-ylmethyl)benzimidazole;1-[(4-chlorophenyl)methyl]-2-(pyrrolidin-1-ylmethyl)benzimidazole;1-[(4-chlorophenyl)methyl]-2-(1-pyrrolidinylmethyl)-1H-benzimidazole
CAS号	442-52-4
分子式	C19H20ClN3
分子量	325.84
EINECS号	207-133-5
相关类别	小分子抑制剂，天然产物;微生物Microbiology;小分子抑制剂;原料药;Inhibitors;API intermediates
Mol文件	442-52-4.mol
结构式

吡咯咪唑 性质

吡咯咪唑 用途与合成方法

用途

吡咯咪唑又叫1-[(4-氯苯基)甲基]-2-(吡咯烷-1-基甲基)苯并咪唑，克立咪唑，具有抗组胺作用，具有中等度的镇静作用及明显的止痒作用。最新研究表明其具有抗丙型肝炎病毒的作用。本品能延长心房肌有效不应期，有治疗房扑的报道。

生物活性

Clemizole是第一代组胺受体(H1 receptor)拮抗剂，是有效的行为性和电生理癫痫活性的抑制剂。它对丙型肝炎的感染具有潜在疗效，能有效地抑制TRPC5离子通道。

靶点

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.

安全信息

MSDS信息

吡咯咪唑 价格(试剂级)

吡咯咪唑 上下游产品信息

上游原料

氢氧化钠乙酸乙酯甲醇二氯甲烷醋酸N,N-二甲基甲酰胺石油醚甲苯三氯氧磷亚硝酸钠硼氢化钠氯化亚锡二水合物对氯苯甲醛氯乙酰氯四氢吡咯2-硝基苯胺对甲苯磺酸水合物邻氯硝基苯邻氯苯甲胺氯化钠