Clemizole is anH1histamine receptorantagonist, is found to substantially inhibitHCVreplication. Clemizole is an inhibitor ofTRPC5 channel. TheIC₅₀of Clemizole for RNA binding byNS4Bis 24±1 nM, whereas itsEC₅₀for viral replication is 8 μM.

IC50: 24 nM (NS4B)^[1]
H1 histamine receptor^[1]

Clemizole hydrochloride is found to inhibit HCV RNA replication in cell culture that is mediated by its suppression of NS4B’s RNA binding, with little toxicity for the host cell. The EC₅₀of Clemizole on the W55R mutant J6/JFH RNA is ~18 μM (2.25 times the EC₅₀of the wild-type RNA)^[1]. Clemizole is a novel inhibitor of TRPC5 channels. Clemizole efficiently blocks TRPC5 currents and Ca²⁺entry in the low micromolar range (IC₅₀=1.0-1.3 μM). Clemizole exhibits a six-fold selectivity for TRPC5 over TRPC4β (IC₅₀=6.4 μM), the closest structural relative of TRPC5, and an almost 10-fold selectivity over TRPC3 (IC₅₀=9.1 μM) and TRPC6 (IC₅₀=11.3 μM). Clemizole hydrochloride as a novel blocker of TRPC5 with a half-maximal inhibitory concentration of 1.1 μM. The concentration-response curves confirmed a concentration-dependent block of TRPC5 by Clemizole and revealed an apparent IC₅₀of 1.1±0.04 μM^[2].

Clemizole hydrochloride has an unexpectedly short plasma half-life (measured at 0.15 hours); it is very rapidly biotransformed into a glucuronide (M14) and a dealkylated metabolite (M12) and into a variety of lesser metabolites in C57BL/6J mice^[3].

325.84

C₁₉H₂₀ClN₃

442-52-4

克立咪唑；吡咯咪唑；克敏唑

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.