CINANSERIN HYDROCHLORIDE

生物活性靶点体外研究体内研究 CINANSERIN HYDROCHLORIDE 试剂级价格

CAS号:54-84-2
英文名:CINANSERIN HYDROCHLORIDE
中文名:CINANSERIN HYDROCHLORIDE
CBNumber:CB2254025
分子式:C20H25ClN2OS
分子量:376.94
MOL File:54-84-2.mol

CINANSERIN HYDROCHLORIDE化学性质

密度 :1.22 g/cm3
储存条件 :Inert atmosphere,Store in freezer, under -20°C
溶解度 :DMSO : 125 mg/mL (331.62 mM; Need ultrasonic)
形态 :Powder
颜色 :Light yellow to yellow
水溶解性 :Soluble to 50 mM in water

安全信息

海关编码 :2921490090

CINANSERIN HYDROCHLORIDE性质、用途与生产工艺

生物活性 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，Ki 为 41 nM。Cinanserin hydrochloride 对 5-HT2 的结合亲和力比对 5-HT1 受体 (Ki 为 3500 nM) 的结合亲和力高得多。Cinanserin hydrochloride 还是严重急性呼吸系统综合症冠状病毒的 3C 样蛋白酶 (3C-like proteinase) 的抑制剂，可大大减少体外的病毒复制。
靶点

5-HT ₂ Receptor

41 nM (Ki)

3C-like proteinase
体外研究

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 IC ₅₀ 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 IC ₅₀ 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.

体内研究

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.

Animal Model:	Male Wistar rats (250 g) underwent thermal injury
Dosage:	5 mg/kg
Administration:	Intravenous injection; for 2 hours
Result:	Significantly reduced systemic burn edema to shamburn levels..