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Clemizole hydrochlorideH1 histamine receptor antagonist

Clemizole hydrochloride

Catalog No. A3316
Size Price Stock Qty
5mg $50.00 In stock
10mg $80.00 In stock
50mg $300.00 In stock
100mg $480.00 In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

Clemizole hydrochloride

Related Biological Data

Clemizole hydrochloride

Biological Activity

Description Clemizole hydrochloride is an antagonist of H1 histamine receptor with an IC50 value of 8 mM for NS4B RNA binding.
Targets NS4B HCV(Hepatitis C Virus)        
IC50 8 mM          

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Chemical Properties

Cas No. 1163-36-6 SDF Download SDF
Chemical Name 1-[(4-chlorophenyl)methyl]-2-(pyrrolidin-1-ylmethyl)benzimidazole;hydrochloride
Canonical SMILES C1CCN(C1)CC2=NC3=CC=CC=C3N2CC4=CC=C(C=C4)Cl.Cl
Formula C19H21Cl2N3 M.Wt 362.3
Solubility Soluble in Water Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

Background

IC50: 8 mM (NS4B)

The NS4B protein is a key player in HCV replication. Disrupting NS4B function thus represents an attractive new anti-HCV strategy. Combining clemizole with other anti-HCV agents could increase the antiviral effect achieved with 1 active drug alone and decrease emergence of viral resistance.

In vitro: Although significant, clemizole’s antiviral effect was moderate (50% effective concentration of 8 mM against a HCV genotype 2a clone). Clemizole’s antiviral effect was highly synergistic with the HCV protease inhibitors VX950 and SCH503034, without toxicity. In contrast, clemizole combinations with either interferon, ribavirin, or the nucleoside (NM283) and nonnucleoside (HCV796) HCV polymerase inhibitors were additive [1].

In vivo: Clemizole had an unexpectedly short plasma half-life; it was very rapidly bio-transformed into a glucuronide (M14) and a dealkylated metabolite (M12) and into a variety of lesser metabolites in C57BL/6J mice [2].

Clinical trial: The purpose of a study was to test the hypothesis that clemizole hydrochloride was safe and well tolerated when administered to subjects who were infected with hepatitis C virus and had not yet received treatment. This clinical study would also examine how the virus and body respond to clemizole hydrochloride (https://clinicaltrials.gov/ct2/show/NCT00945880?term=Clemizole&rank=1).

References:
[1] Einav S, Sobol HD, Gehrig E, Glenn JS.  The hepatitis C virus (HCV) NS4B RNA binding inhibitor clemizole is highly synergistic with HCV protease inhibitors. J Infect Dis. 2010;202(1):65-74.
[2] Nishimura T, Hu Y, Wu M, Pham E, Suemizu H, Elazar M, Liu M, Idilman R, Yurdaydin C, Angus P, Stedman C, Murphy B, Glenn J, Nakamura M, Nomura T, Chen Y, Zheng M, Fitch WL, Peltz G.  Using chimeric mice with humanized livers to predict human drug metabolism and a drug-drug interaction. J Pharmacol Exp Ther. 2013;344(2):388-96. doi: 10.1124/jpet.112.198697. Epub 2012 Nov 8.