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Clemizole hydrochloride

CAS No. : 1163-36-6

MCE 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。

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

作用靶点：Histamine Receptor  |  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 ?M (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 ?M). Clemizole exhibits a six-fold selectivity for TRPC5 over TRPC4β (IC₅₀=6.4 ?M), the closest structural relative of TRPC5, and an almost 10-fold selectivity over TRPC3 (IC₅₀=9.1 ?M) and TRPC6 (IC₅₀=11.3 ?M). Clemizole hydrochloride as a novel blocker of TRPC5 with a half-maximal inhibitory concentration of 1.1 ?M. The concentration-response curves confirmed a concentration-dependent block of TRPC5 by Clemizole and revealed an apparent IC₅₀ of 1.1±0.04 ?M.

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.

相关产品：Drug Repurposing Compound Library Plus  |  FDA-Approved Drug Library Plus  |  FDA-Approved Drug Library Mini  |  Bioactive Compound Library Plus  |  Anti-Infection Compound Library  |  GPCR/G Protein Compound Library  |  Immunology/Inflammation Compound Library  |  Metabolism/Protease Compound Library  |  Neuronal Signaling Compound Library  |  FDA-Approved Drug Library  |  Anti-Cancer Compound Library  |  Antiviral Compound Library  |  Drug Repurposing Compound Library  |  Endocrinology Compound Library  |  Orally Active Compound Library  |  Neurotransmitter Receptor Compound Library  |  FDA Approved & Pharmacopeial Drug Library  |  Anti-Hepatitis C Virus Compound Library  |  Resiquimod  |  Honokiol  |  Ribavirin  |  Deferiprone  |  U18666A  |  AG-1478  |  EIDD-1931  |  Histamine  |  Artemisinin  |  NIM811  |  Alisporivir  |  Clemastine fumarate  |  Myriocin  |  Mizoribine  |  Merimepodib  |  Amitriptyline hydrochloride  |  Astemizole  |  Fexofenadine hydrochloride  |  Osthole  |  Terfenadine  |  Famotidine  |  Diphenhydramine hydrochloride  |  Levocetirizine dihydrochloride  |  Perphenazine  |  Loratadine  |  NHC-triphosphate  |  PSI-7409  |  Cimetidine  |  Peretinoin  |  Chlorprothixene

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