| Bioactivity | Cinanserin hydrochloride (SQ 10643) is a potent, selective and highly affinity 5-HT2 receptor antagonist with a Ki of 41 nM. Cinanserin hydrochloride has a much higher binding affinity for the 5-HT2 than for the 5-HT1 receptor (Ki of 3500 nM). Cinanserin is also an inhibitor of 3C-like proteinase of severe acute respiratory syndrome coronavirus and strongly reduces virus replication in vitro[1][2][3]. |
| Invitro | Cinanserin/Cinanserin hydrochloride have binding affinity to SARS-CoV 3CLpro, HCoV-229E 3CLpro, with the KD values of 49.4 μM/78.0 μM for SARS-associated coronavirus (SARS-CoV) 3CLpro and 18.2 μM/36.6 μM for human coronavirus 229E (HCoV-229E) 3CLpro[1].The IC50 values of Cinanserin and Cinanserin hydrochloride for inhibiting the catalytic activity of SARS-CoV 3CLpro are calculated as 4.92 μM and 5.05 μM, respectively, The corresponding IC50 values for HCoV-229E 3CLpro are 4.68 μM and 5.68 μM. None of the compounds have inhibitory activity against HRV-14 3Cpro at concentrations up to 200 μM[1]. |
| 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[2]. Animal Model: |
| Name | Cinanserin hydrochloride |
| CAS | 54-84-2 |
| Formula | C20H25ClN2OS |
| Molar Mass | 376.94 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| Reference | [1]. Chen L, et al. Cinanserin is an inhibitor of the 3C-like proteinase of severe acute respiratory syndrome coronavirus and strongly reduces virus replication in vitro. J Virol. 2005 Jun;79(11):7095-103. [2]. Hernekamp JF, et al. Cinanserin reduces plasma extravasation after burn plasma transfer in rats. Burns. 2013 Sep;39(6):1226-33. [3]. Leysen JE, et al. Receptor binding profile of R 41 468, a novel antagonist at 5-HT2 receptors. Life Sci. 1981 Mar 2;28(9):1015-22. |
Cinanserin hydrochloride
CAS: 54-84-2 F: C20H25ClN2OS W: 376.94
Cinanserin hydrochloride (SQ 10643) is a potent, selective and highly affinity 5-HT2 receptor antagonist with a Ki of 41
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