1-[(4-氯苯基)甲基]-2-(吡咯烷-1-基甲基)苯并咪唑鹽酸鹽

生物活性靶點(diǎn)體外研究體內(nèi)研究 用途與合成方法 MSDS 1-[(4-氯苯基)甲基]-2-(吡咯烷-1-基甲基)苯并咪唑鹽酸鹽價(jià)格(試劑級(jí)) 上下游產(chǎn)品信息

中文名稱	1-[(4-氯苯基)甲基]-2-(吡咯烷-1-基甲基)苯并咪唑鹽酸鹽
中文同義詞	1-[(4-氯苯基)甲基]-2-(吡咯烷-1-基甲基)苯并咪唑鹽酸鹽;1-對(duì)氯芐基-2-(1-吡咯烷基)甲基苯并咪唑 鹽酸鹽;克立咪唑鹽酸;鹽酸克立咪唑, >98%;鹽酸克立咪唑;鹽酸氯咪唑;克立咪唑鹽酸鹽;1-(4-氯芐基)-2-(吡咯烷-1-基甲基)-1H-苯并[D]咪唑鹽酸鹽
英文名稱	Clemizole hydrochloride
英文同義詞	1-[(4-Chlorophenyl)methyl]-2-(1-pyrrolidinylmethyl)-1H-benzimidazole hydrochloride;1-[(4-chlorophenyl)methyl]-2-(pyrrolidin-1-ylmethyl)benzimidazole,hydrochloride;CS-1763;allercur;allercurehydrochloride;p48;1-P-CHLOROBENZYL-2-[1-PYRROLIDINYL]-METHYLBENZIMIDAZOLE HYDROCHLORIDE;1-[(4-Chlorophenyl)methyl]-2-(pyrrolidin-1-ylmethyl)benzoimidazole hydrochloride
CAS號(hào)	1163-36-6
分子式	C19H21Cl2N3
分子量	362.3
EINECS號(hào)	214-605-4
相關(guān)類別	抑制劑;小分子抑制劑;小分子抑制劑，天然產(chǎn)物;Inhibitors
Mol文件	1163-36-6.mol
結(jié)構(gòu)式

1-[(4-氯苯基)甲基]-2-(吡咯烷-1-基甲基)苯并咪唑鹽酸鹽 性質(zhì)

1-[(4-氯苯基)甲基]-2-(吡咯烷-1-基甲基)苯并咪唑鹽酸鹽 用途與合成方法

生物活性

Clemizole hydrochloride 是一種 H1 組胺受體 (H1 histamine receptor) 拮抗劑，抑制 HCV 復(fù)制。

靶點(diǎn)

IC50: 24 nM (NS4B)  
 H1 histamine receptor

體外研究

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.

體內(nèi)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.

用途 

用作氯咪唑青霉素等藥物的中間體

安全信息

MSDS信息

1-[(4-氯苯基)甲基]-2-(吡咯烷-1-基甲基)苯并咪唑鹽酸鹽 價(jià)格(試劑級(jí))

1-[(4-氯苯基)甲基]-2-(吡咯烷-1-基甲基)苯并咪唑鹽酸鹽 上下游產(chǎn)品信息

上游原料

鄰氯硝基苯鄰氯苯甲胺氯乙酰氯四氫吡咯氯化鈉