盐酸伊伐布雷定

中文名称:

盐酸伊伐布雷定

中文同义词:

盐酸伊伐布雷啶;盐酸伊伐布雷定IVABRADINE(研发中);盐酸伊伐布雷定及中间体;盐酸伊伐布雷定(依法布雷定);依伐布雷定盐酸盐;盐酸依伐布雷定;盐酸伊伐布雷;盐酸伊伐布雷定/盐酸依法布雷定

英文名称:

Ivabradine hydrochloride

英文同义词:

Ivabradine HCl;Ivabradine hydrochloride;3-[3-[[(8S)-3,4-Dimethoxy-8-bicyclo[4.2.0]octa-1,3,5-trienyl]methyl-methylamino]propyl]-7,8-dimethoxy-2,5-dihydro-1H-3-benzazepin-4-one hydrochloride;Ivabradine hydrochloride, >=99%;IVABRADINE HYDROCHLORIDE-OTHER COMPOUNDSCONTAINING AN UNFUSED PYRAZOLE RING(WHETHER OR NOT HYDROGENATED)IN THE STRUCTUR;Ivabradine hydrochloride, 98%, a If inhibitor;3-[3-[[[(7S)-3,4-Dimethoxybicyclo[4.2.0]octa-1,3,5-trien-7-yl]methyl]methylamino]propyl]-1,3,4,5-tetrahydro-7,8-dimethoxy-2H-3-benzazepin-2-one Hydrochloride;Corlentor

CAS号:

148849-67-6

分子式:

C27H36N2O5.HCl

分子量:

505.05

EINECS号:

638-798-3

相关类别:

小分子抑制剂，天然产物;医药原料药;医药原料;医药中间体;原料药;小分子抑制剂;神经信号;细胞生物学试剂;Intermediates Fine Chemicals;Pharmaceuticals;API;Chiral Reagents;Heterocycles;Cardiovascular APIs;Inhibitors;心脏;药物杂质及中间体;原料;医药、农药及染料中间体;医药化工类

Mol文件:

148849-67-6.mol

熔点 

193-196?C

比旋光度 

58921 +7.8°; 36521 +27.8° (c = 1% in DMSO)

储存条件 

-20°C Freezer

溶解度 

H2O: ≥5mg/mL (warmed)

形态

powder

颜色

white to beige

旋光性 (optical activity)

[α]/D +5 to +9°, c = 1 in DMSO

Merck 

14,5247

InChIKey

HLUKNZUABFFNQS-ZMBIFBSDSA-N

CAS 数据库

148849-67-6(CAS DataBase Reference)

用途

盐酸伊伐布雷定是首个选择性和特异性调节心率抑制剂,对窦房结有选择性作用而对心脏内传导、心肌收缩或心室复极化无作用。

用途

盐酸伊伐布雷定是依瓦拉定与一摩尔等量的盐酸合成的盐酸盐，用于治疗不能耐受-受体阻滞剂和/或心力衰竭的心绞痛患者。

生物活性

Ivabradine HCl (S 16257-2)是一种新型If抑制剂，IC50为2.9 μM，特定有效作用于窦房结心脏起搏器活性，是一种纯粹的心跳速率降低剂。

靶点

Target Value Adrenergic Receptor

Target

Value

Adrenergic Receptor

体内研究

Ivabradine hydrochloride treatment (10 mg/kg/d) induces long-term HRR, and that improves diastolic LV function probably involving attenuated hypoxia, reduced remodeling, and/or preserved nitric oxide bioavailability, resulting from processes triggered early after HRR initiation: angiogenesis and/or preservation of endothelial nitric oxide synthase expression. Ivabradine hydrochloride leads to a sustained 15-20% heart rate reduction, but has no effect on blood pressure. While ivabradine has no effect on endothelial function and vascular reactive oxygen species production in angiotensin II-treated rats, it improves both parameters in ApoE knockout mice. Ivabradine hydrochloride treatment leads to an attenuation of angiotensin II signaling and increased the expression of telomere-stabilizing proteins in ApoE knockout mice, which may explain its beneficial effects on the vasculature. The absence of these protective ivabradine effects in angiotensin II-infused rats may relate to the treatment duration or the presence of arterial hypertension.