Clemizole | 吡咯咪唑 | MedChemExpress (MCE)

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Clemizole

CAS No. : 442-52-4

MCE 国际站：Clemizole

产品活性：Clemizole 是 H1 受体拮抗剂，还能抑制 NS4B 的 RNA 结合及 HCV 的复制。Clemizole也是一种 TRP5 通道的抑制剂。

研究领域：GPCR/G Protein  |  Neuronal Signaling  |  Immunology/Inflammation  |  Membrane Transporter/Ion Channel  |  Metabolic Enzyme/Protease  |  Anti-infection

作用靶点：Histamine Receptor  |  TRP Channel  |  HCV Protease  |  HCV

In Vitro: 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 EC₅₀ of Clemizole on the W55R mutant J6/JFH RNA is ~18 µM (2.25 times the EC₅₀ of the wild-type RNA). 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 IC₅₀ of 1.1±0.04 µM.

In Vivo: 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.

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