Clemizole hydrochloride | 盐酸克立咪唑 | MedChemExpress (MCE)
品牌 | 厂商性质 | 产地 | 货期 | 价格 |
---|---|---|---|---|
MedChemExpress (MCE) | 生产商 | 美国 | 现货 | 550 |
性能特点
Clemizole hydrochloride 是一种 H1 组胺受体 (H1 histamine receptor) 拮抗剂,抑制 HCV 复制。Clemizole hydrochlorid
规格 | CAS号 | 价格 | 操作 |
---|---|---|---|
10 mM * 1 mL | 1163-36-6 | ¥550.00 | 询底价 |
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Clemizole hydrochloride
CAS No. : 1163-36-6
MCE 国际站:Clemizole hydrochloride
产品活性:Clemizole hydrochloride 是一种 H1 组胺受体 (H1 histamine receptor) 拮抗剂,抑制 HCV 复制。Clemizole hydrochloride 还是一种 TRPC5 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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