|1-(4-氯苄基)-2-(吡咯烷-1-基甲基)-1H-苯并[d]咪唑盐酸盐|CsnPharm

CAS No.: 1163-36-6

Clemizole HCl/盐酸克立咪唑 Catalog No. CSN10665

Synonyms: Clemizole (hydrochloride);AL 20;Allercur

Clemizole HCl is an H1 histamine receptor antagonist, is found to substantially inhibit HCV replication. The IC50 of Clemizole for RNA binding by NS4B is 24±1 nM, whereas its EC50 for viral replication is 8 µM.

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描述Clemizole HCl, an H1 histamine receptor antagonist, is found to substantially inhibit HCV replication. The IC50 of Clemizole for RNA binding by NS4B is 24±1 nM, whereas its EC50 for viral replication is 8 µM. The EC50 of Clemizole on the W55R mutant J6/JFH RNA is ~18 µM (2.25 times the EC50 of the wild-type RNA)^[1]. Clemizole is a novel inhibitor of TRPC5 channels. Clemizole efficiently blocks TRPC5 currents and Ca2+ entry in the low micromolar range (IC50=1.0-1.3 µM). Clemizole exhibits a six-fold selectivity for TRPC5 over TRPC4β (IC50=6.4 µM), the closest structural relative of TRPC5, and an almost 10-fold selectivity over TRPC3 (IC50=9.1 µM) and TRPC6 (IC50=11.3 µM). Clemizole decreased hERG current by blocking both open and closed states of the channel in a concentration-dependent manner (IC50 : 0.07 μM). Clemizole also moderately decreased IKs and human Kv 1.5 channel current. Moreover, clemizole increased the duration of the ventricular action potential in guinea pig hearts and the QTc interval in isolated perfused hearts from guinea pigs, in a concentration-dependent manner (0.1-1.0 μM)^[2]. Clemizole HCl 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^[3].
临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT00945880	Hepatitis C	Phase 1	Completed	-	-
NCT03069508	Hepatocellular Carcinoma	Phase 2	Enrolling by invitation	January 31, 2018	Turkey ... more >> University of Ankara Ankara, Turkey Collapse <<
NCT00945880	Hepatitis C	Phase 1	Completed	-	-

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.7602 mL
- 13.8009 mL
- 27.6017 mL
- 5 mM
- 0.5520 mL
- 2.7602 mL
- 5.5203 mL
- 10 mM
- 0.2760 mL
- 1.3801 mL
- 2.7602 mL

技术信息

CAS号

1163-36-6

储存条件

粉末: Inert atmosphere,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C19H21Cl2N3

运输

蓝冰

分子量

362.30

别名

Clemizole (hydrochloride);AL 20;Allercur;P 48;Reactrol;Clemizole;盐酸克立咪唑

溶解度

DMSO	175.0 mg/mL (483.0 mM)
Water	insoluble

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Clemizole HCl/盐酸克立咪唑 Catalog No. CSN10665

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