|1-[(4-氯苯基)甲基]-2-(吡咯烷-1-基甲基)苯并咪唑|CsnPharm

CAS No.: 442-52-4

Clemizole/吡咯咪唑 Catalog No. CSN10664

Synonyms: NSC-46261;吡咯咪唑

Clemizole is an antagonist of H1 histamine receptor that can inhibit NS4B's RNA binding and hepatitis C virus (HCV) replication.

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技术信息

生物活性

描述Clemizole, a histamine H1 receptor antagonist has a potential therapeutic effect on hepatitis C infection and also potently inhibits TRPC5 ion channels. 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)^[3]. Clemizole binds to serotonin receptors and its antiepileptic activity can be mimicked by drugs acting on serotonin signalling pathways e.g. trazodone and lorcaserin^[4]. Clemizole efficiently blocks TRPC5 currents and Ca(2+) entry in the low micromolar range (IC50 = 1.0 - 1.3 µM), as determined by fluorometric intracellular free Ca(2+) concentration ([Ca(2+)]i) measurements and patch-clamp recordings. Moreover, clemizole was still effective in blocking TRPC5 single channels in excised inside-out membrane patches, hinting to a direct block of TRPC5 (Canonical transient receptor potential channel 5) by clemizole^[5].
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 <<

参考文献

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
- 3.0690 mL
- 15.3452 mL
- 30.6904 mL
- 5 mM
- 0.6138 mL
- 3.0690 mL
- 6.1381 mL
- 10 mM
- 0.3069 mL
- 1.5345 mL
- 3.0690 mL

技术信息

CAS号

442-52-4

储存条件

粉末: Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C19H20ClN3

运输

蓝冰

分子量

325.84

别名

NSC-46261;吡咯咪唑

溶解度

DMSO	65.0 mg/mL (199.5 mM)

动物实验配方

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