54-84-2

中文名称 CINANSERIN HYDROCHLORIDE

英文名称 CINANSERIN HYDROCHLORIDE

CAS 54-84-2

分子式 C20H25ClN2OS

分子量 376.94

MOL 文件 54-84-2.mol

更新日期 2023/03/20 15:41:23

54-84-2 结构式

基本信息物理化学性质安全数据图谱信息常见问题列表

基本信息

中文别名

N-(2-((3-(二甲氨基)丙基)硫代)苯基)-3-苯基丙烯酰胺盐酸盐

英文别名

DPTC
maptc
sq10,643
Nsc125717
CINANSERIN
Cinnanserin
DPTC HYDROCHLORIDE
CINANSERIN HYDROCHLORIDE
2'-(3-DIMETHYLAMINOPROPYL-THIO)-CINNAMANILIDE HYDROCHLORIDE
DPTC 2'-(3-Dimethylaminopropylthio)cinnamanilide hydrochloride

物理化学性质

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)

形态粉末

颜色Light yellow to yellow

水溶解性Soluble to 50 mM in water

安全数据

危险性符号(GHS) GHS hazard pictograms

GHS07

警示词警告

危险性描述H302-H315-H319-H335

防范说明P261-P280-P301+P312-P302+P352-P305+P351+P338

海关编码2921490090

图谱信息

CINANSERIN HYDROCHLORIDE(54-84-2)核磁图(¹HNMR)

常见问题列表

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..