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Clemizole hydrochloride | 盐酸克立咪唑 | MedChemExpress (MCE)

英文名称:Clemizole hydrochloride
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

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产品参数
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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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