Clemizole

• CAT Number: I003565
• CAS Number: 442-52-4
• Molecular Formula: C19H20ClN3
• Molecular Weight: 325.84
• Purity: ≥95%
• Synonyms: 1-[(4-chlorophenyl)methyl]-2-(pyrrolidin-1-ylmethyl)benzimidazole
• Target: Histamine Receptor
• Solubility: 10 mM in DMSO
• Storage: Store at -20°C
• IC50: 8 mM (NS4B) [1]

Clemizole is a H1 histamine receptor antagonist.Recently, researchers have identified that clemizole hydrochloride can inhibit NS4B/’s RNA binding and hepatitis C virus (HCV) replication.IC50 Value: 8 mM (NS4B) [1]Target: H1 receptor; Anti-HCVin vitro: Although significant, clemizole/’s antiviral effect is moderate (50% effective concentration of 8 microM against an HCV genotype 2a clone). Combinations of clemizole with either interferon, ribavirin, or the nucleoside (NM283) and nonnucleoside (HCV796) HCV polymerase inhibitors were additive [1]. The differences in the rodent and human pathways for clemizole metabolism were of importance, because the predominant human metabolite was found to have synergistic anti-HCV activity [2].in vivo: Clemizole and reserpine treatment did not produce any modification of the dose-response curve to histamine [3].Clinical trial: Safety and Tolerability Study of Clemizole Hydrochloride to Treat Hepatitis C in Subjects Who Are Treatment-Naive (CLEAN-1). NCT00945880. Phase 1

Reference

[1]. Einav S, Sobol HD, Gehrig E, The hepatitis C virus (HCV) NS4B RNA binding inhibitor clemizole is highly synergistic with HCV protease inhibitors. J Infect Dis. 2010 Jul 1;202(1):65-74.
[2]. Nishimura T, Hu Y, Wu M, Using chimeric mice with humanized livers to predict human drug metabolism and a drug-drug interaction.J Pharmacol Exp Ther. 2013 Feb;344(2):388-96.
[3]. Martínez-Mir I, Herrero J, Esta? L, Effect of histamine on the longitudinal and circular muscle of the oestrogen dominated rat uterus. Agents Actions. 1993 May;39(1-2):1-5.