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Ivabradine hydrochloride
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
CAS NO:148849-67-6
包装与价格:
包装价格(元)
10 mg电议
100 mg电议
1 mL*10 mM(in DMSO)电议

产品名称
S 16257-2
盐酸伊伐布雷定
Ivabradine HCl
产品介绍
Ivabradine hydrochloride 是一种可口服的,超极化激活的环核苷酸门控离子通道通道阻滞剂。

产品描述

Ivabradine hydrochloride is a new If inhibitor (IC50: 2.9 μM). Ivabradine Hydrochloride is the hydrochloride salt form of ivabradine, an orally bioavailable, hyperpolarization-activated, cyclic nucleotide-gated (HCN) channel blocker, with negative chronotropic activity. Upon administration, ivabradine selectively binds to the intracellular portion of the HCN channel pore and blocks HCN channels in the pacemaker cells within the sinoatrial (SA) node. This inhibits the If (funny) pacemaker ion current, prevents the inward flow and intracellular accumulation of positively charged ions, reduces pacemaker activity and slows diastolic depolarization.

体内活性

Ivabradine 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[1]. Ivabradine causes 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 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[2].

Cas No.

148849-67-6

分子式

C27H37ClN2O5

分子量

505.05

别名

S 16257-2;盐酸伊伐布雷定;Ivabradine HCl

储存和溶解度

H2O:75 mg/mL (148.5 mM)
Ethanol:93 mg/mL (184.1 mM)
DMSO:93 mg/mL (184.1 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years