91940-87-3

中文名称 ZATEBRADINE HCL

英文名称 3-[3-[[2-(3,4-DIMETHOXYPHENYL)ETHYL]METHYLAMINO]PROPYL]-1,3,4,5-TETRAHYDRO-7,8-DIMETHOXY-2H-3-BENZAZEPIN-2-ONE HYDROCHLORIDE

CAS 91940-87-3

分子式 C26H37ClN2O5

分子量 493.04

MOL 文件 91940-87-3.mol

91940-87-3 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

盐酸扎替雷定

英文别名

UL-FS49
ULFS 49CL
Zatebradine HCl
ZATEBRADINE HYDROCHLORIDE
Zatebradine dihydrochloride
3-(3-((3,4-dimethoxyphenethyl)(methyl)amino)propyl)-7,8-dimethoxy-4,5-dihydro-1H-benzo[d]azepin-2(3H)-one hydrochloride
3-[3-[[2-(3,4-DIMETHOXYPHENYL)ETHYL]METHYLAMINO]PROPYL]-1,3,4,5-TETRAHYDRO-7,8-DIMETHOXY-2H-3-BENZAZEPIN-2-ONE HYDROCHLORIDE
7,8-Dimethoxy-3-[3-[-N-[2-(3,4 dimethoxyphenyl)ethyl]-N-methylamino]propyl]-1,3,4,5-tetrahydro-2H-3-benzazepin-2-one hydrochloride
2H-3-Benzazepin-2-one, 3-(3-((2-(3,4-dimethoxyphenyl)ethyl)methylamino)propyl)-1,3,4,5-tetrahydro-7,8-dimethoxy-, monohydrochloride
UL-FS49, 3-[3-[[2-(3,4-Dimethoxyphenyl)ethyl]methylamino]propyl]-1,3,4,5-tetrahydro-7,8-dimethoxy-2H-3-benzazepin-2-one hydrochloride

物理化学性质

熔点188° and mp 168°

储存条件2-8°C

溶解度H₂O: ~14 mg/mL

溶解度在水中的溶解度~14 mg/mL

形态solid

颜色white

水溶解性Soluble in water (100mM)

安全数据

安全说明22-24/25

WGK Germany3

图谱信息

ZATEBRADINE HCL(91940-87-3)核磁图(¹HNMR)

常见问题列表

生物活性

Zatebradine (UL-FS-49 (free base)) 是一种高效的 HCN Channel 抑制剂，其 IC50 值为 1.96 µM。Zatebradine 会阻止通过人类 HCN1，HCN2，HCN3 和 HCN4 通道的缓慢内向电流，其 IC50 值分别为 1.83 µM，2.21 µM，1.90 µM 和 1.88 µM。

靶点

IC50: 1.96 µM ( HCN channels )

体外研究

The use-dependent blockade by Zatebradine of the cardiac pacemaker current from rabbit sino-atrial node cells has an apparent K _d of 480 nM.

体内研究

Zatebradine (0-20 mg/kg; intraperitoneal injection; for 30 minutes; male C57/Bl6-mice) reduces the heart rate dose-dependently from 600 to 200 bpm with ED ₅₀ value of 1.8 mg/kg and induces increasing arrhythmia.

Animal Model:	Male C57/Bl6-mice
Dosage:	0 mg/kg, 0.1 mg/kg, 1 mg/kg, 10 mg/kg, 20 mg/kg
Administration:	Intraperitoneal injection; for 30 minutes
Result:	Observed acute blood glucose reduction, dose-dependently reduced glycated hemoglobin, significantly prevented the decrease of IRI levels at doses of 3 and 10 mg/kg, and no difference in food intake or body weight.