91940-87-3
中文名稱
ZATEBRADINE HCL
英文名稱
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
更新日期
2024/12/03 15:40:31
91940-87-3 結(jié)構(gòu)式
基本信息
中文別名
鹽酸扎替雷定 英文別名
UL-FS49ULFS 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
物理化學(xué)性質(zhì)
熔點(diǎn)188° and mp 168°
儲(chǔ)存條件2-8°C
溶解度H2O: ~14 mg/mL
溶解度在水中的溶解度~14 mg/mL
形態(tài)solid
顏色white
水溶解性Soluble in water (100mM)
常見(jiàn)問(wèn)題列表
生物活性
Zatebradine (UL-FS-49 (free base)) 是一種高效的 HCN Channel 抑制劑，其 IC50 值為 1.96 μM。Zatebradine 會(huì)阻止通過(guò)人類 HCN1，HCN2，HCN3 和 HCN4 通道的緩慢內(nèi)向電流，其 IC50 值分別為 1.83 μM，2.21 μM，1.90 μM 和 1.88 μM。靶點(diǎn)
IC50: 1.96 μM ( HCN channels )
體外研究
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.
體內(nèi)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. |