Clemizole hydrochloride

• CAT Number: I000589
• CAS Number: 1163-36-6
• Molecular Formula: C19H20ClN3 • HCl
• Molecular Weight: 362.3
• Purity: ≥95%
• Synonyms: AL 20;Allercur
• Target: H1 receptor; Anti-HCV
• Solubility: DMSO: ≥ 3.6 mg/mL
• Storage: -20°C
• IC50: 8mM (NS4B)
• IUPAC Name: 1-[(4-chlorophenyl)methyl]-2-(pyrrolidin-1-ylmethyl)benzimidazole;hydrochloride
• InChI: InChI=1S/C19H20ClN3.ClH/c20-16-9-7-15(8-10-16)13-23-18-6-2-1-5-17(18)21-19(23)14-22-11-3-4-12-22;/h1-2,5-10H,3-4,11-14H2;1H
• InChIKey: DNFMJYXRIMLMBZ-UHFFFAOYSA-N
• SMILES: C1CCN(C1)CC2=NC3=CC=CC=C3N2CC4=CC=C(C=C4)Cl.Cl

Clemizole hydrochloride (CAT: I000589) is a pharmaceutical compound that acts as an antihistamine and a modulator of ion channels. It was initially developed as an antihistamine, primarily targeting the H1 histamine receptor. By blocking the H1 receptor, clemizole hydrochloride inhibits the effects of histamine, such as allergic reactions and itching. However, it has also been found to modulate other ion channels, including TRPC5 and TPRM7. These ion channels play roles in various physiological processes, including neuronal signaling and sensory perception. The modulation of ion channels by clemizole hydrochloride may contribute to its potential therapeutic applications beyond its antihistamine effects.

Overview of Clinical Research

Clemizole is a Hepatitis C virus NS4 protein inhibitor. The Phase-II for Liver cancer discontinued in Turkey (PO) (Eiger BioPharmaceuticals pipeline, September 2020)

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.