货号 | 17695-1mg |
描述 | Clemizole is an antihistamine that antagonizes the histamine 1 receptor at high nanomolar concentrations.1,2 It less potently blocks transient receptor potential canonical channel 5 (TRPC5; IC50 = 1.0-1.3 µM), with at least 6-fold selectivity for TRPC5 over other TRP channels.3 Clemizole also has hepatitis C antiviral action through inhibition of NS4B function, showing synergy with boceprevir (Item No. 18379), and it inhibits seizures in a zebrafish model of Dravet Syndrome.4,5 |
别名 | AL 20;Allercur; |
供应商 | Cayman |
应用文献 | |
1.Aguilar, M.J.,Morales-Olivas, F.J., and Rubio, E. Pharmacological investigation into the effects of histamine and histamine analogues on guinea-pig and rat colon in vitro. British Journal of Pharmacology 88(3), 501-506 (1986). 2.Cortijo, J.,Sanz, C.,Perpiña, M., et al. Responses to histamine and selective H2-receptor agonists in lung parenchymal strips from normal and sensitized guinea-pigs. Agents and Actions 28(1-2), 45-52 (1989). 3.Richter, J.M.,Schaefer, M., and Hill, K. Clemizole hydrochloride is a novel and potent inhibitor of transient receptor potential channel TRPC5. Molecular Pharmacology 86(5), 514-521 (2014). 4.Einav, S.,Sobol, H.D.,Gehrig, E., et al. The hepatitis C virus (HCV) NS4B RNA binding inhibitor clemizole is highly synergistic with HCV protease inhibitors. Journal of Infectious Diseases 202(1), 65-74 (2010). 5.Baraban, S.C.,Dinday, M.T., and Hortopan, G.A. Drug screening in Scn1a zebrafish mutant identifies clemizole as a potential Dravet syndrome treatment. Nat.Commun. 4:2410, (2013). | |
运输条件 | Room temperature in continental US; may vary elsewhere |
存放说明 | -20 |
纯度 | ≥98% |
计算分子量 | 362.3 |
分子式 | C19H20ClN3 • HCl |
CAS号 | 1163-36-6 |
稳定性 | ≥ 2 years |
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