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Cinanserin hydrochloride

CAS No. : 54-84-2

MCE 国际站：Cinanserin hydrochloride

产品活性：Cinanserin hydrochloride (SQ 10643) 是一种有效，选择性和高度亲和力的 5-HT₂ 受体拮抗剂，K_i 为 41 nM。Cinanserin hydrochloride 对 5-HT₂ 的结合亲和力比对 5-HT₁ 受体 (K_i 为 3500 nM) 的结合亲和力高得多。Cinanserin hydrochloride 还是COVID-19 病毒的 3C 样蛋白酶 (3C-like proteinase) 的抑制剂，可大大减少体外的病毒复制。

研究领域：GPCR/G Protein  |  Neuronal Signaling  |  Anti-infection

作用靶点：5-HT Receptor  |  Influenza Virus

In Vitro: Cinanserin/Cinanserin hydrochloride have binding affinity to SARS-CoV 3CL^pro, HCoV-229E 3CL^pro, with the K_D values of 49.4 μM/78.0 μM for SARS-associated coronavirus (SARS-CoV) 3CL^pro and 18.2 μM/36.6 μM for human coronavirus 229E (HCoV-229E) 3CL^pro.
The IC₅₀ values of Cinanserin and Cinanserin hydrochloride for inhibiting the catalytic activity of SARS-CoV 3CL^pro are calculated as 4.92 μM and 5.05 μM, respectively, The corresponding IC₅₀ values for HCoV-229E 3CL^pro are 4.68 μM and 5.68 μM. None of the compounds have inhibitory activity against HRV-14 3C^pro at concentrations up to 200 μM.

In Vivo: Cinanserin (5 mg/kg; intravenous injection; for 2 hours; male Wistar rats) treatment significantly reduces systemic burn edema to shamburn levels. Leukocyte-endothelial interactions are significantly reduced by administration of Cinanserin.

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