扎替雷定
|
|
|
- CAS号:
- 85175-67-3
- 英文名:
- Zatebradine
- 英文别名:
- Zatebradine;UL-FS-49 free base;UL-FS-49CL free base;Zatebradine (UL-FS-49;3-(3-((3,4-Dimethoxyphenethyl)(methyl)amino)propyl)-7,8-dimethoxy-4,5-dihydro-1H-benzo[d]azepin-2(3H)-one;2H-3-Benzazepin-2-one, 3-[3-[[2-(3,4-dimethoxyphenyl)ethyl]methylamino]propyl]-1,3,4,5-tetrahydro-7,8-dimethoxy-
- 中文名:
- 扎替雷定
- 中文别名:
- 扎替雷定;化合物 T13387;3-(3-((3,4-二甲氧基苯乙基)(甲基)氨基)丙基)-7,8-二甲氧基-4,5-二氢-1H-苯并[D]氮杂卓-2(3H)-酮
- CBNumber:
- CB11117164
- 分子式:
- C26H36N2O5
- 分子量:
- 456.58
- MOL File:
- 85175-67-3.mol
|
|
|
扎替雷定化学性质
-
沸点:
-
612.5±55.0 °C(Predicted)
-
|
-
密度:
-
1.115±0.06 g/cm3(Predicted)
-
|
-
储存条件:
-
2-8°C
-
|
-
溶解度:
-
DMSO : ≥ 50 mg/mL (109.51 mM)
-
|
-
酸度系数(pKa):
-
8.99±0.50(Predicted)
-
|
扎替雷定性质、用途与生产工艺
Zatebradine (UL-FS-49 (free base); UL-FS-49CL (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。
.
IC50: 1.96 µM (
HCN channels
)
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.
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.
|
扎替雷定
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/01/25 | HY-13422A | 扎替雷定
Zatebradine | 85175-67-3 | 5mg | 990元 |
| 2024/01/25 | HY-13422A | 扎替雷定
Zatebradine | 85175-67-3 | 10mM * 1mLin DMSO | 1089元 |
85175-67-3, 扎替雷定 相关搜索:
- C26H36N2O5
- 化合物 T13387
- 3-(3-((3,4-二甲氧基苯乙基)(甲基)氨基)丙基)-7,8-二甲氧基-4,5-二氢-1H-苯并[D]氮杂卓-2(3H)-酮
- 扎替雷定
- 85175-67-3
- Zatebradine (UL-FS-49
- 3-(3-((3,4-Dimethoxyphenethyl)(methyl)amino)propyl)-7,8-dimethoxy-4,5-dihydro-1H-benzo[d]azepin-2(3H)-one
- 2H-3-Benzazepin-2-one, 3-[3-[[2-(3,4-dimethoxyphenyl)ethyl]methylamino]propyl]-1,3,4,5-tetrahydro-7,8-dimethoxy-
- UL-FS-49CL free base
- UL-FS-49 free base
- Zatebradine