产品名称

Ivabradine HCl(盐酸伊伐布雷定)

一般描述

Ivabradine HCl a new If inhibitor with IC 50 of 2.9 μM which acts specifically on the pacemaker activity of the sinoatrial node, is a pure heart rate lowering agent.

别 称

S16257-2

纯 度

≥98.0%(HPLC)

CAS NO.

148849-67-6

分子式

C²⁷H³⁷ClN²O⁵

分子量

505.052

适用范围

生物试剂，适用于细胞培养等

l  理化信息

外 观

白色至米白色粉末

溶解性(25°C)

DMSO

≥50mg/mL

乙醇

≥50mg/mL

水

≥50mg/mL

l  生物学信息

生物活性/药理作用

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. This decreases heart rate, reduces myocardial oxygen demand and allows more time for blood to flow to the myocardium without affecting cardiac contractility. HCN channels, mixed sodium (Na₊) and potassium (K₊) channels that carry the inward If current, play a key role in the regulation of pacemaker firing rate in the SA node. The If pacemaker current, the inward flow of positively charged Na₊-K₊ ions, initiates the spontaneous diastolic depolarization phase and modulating heart rate.

l  存储

存储温度

-20°C

l  注意事项及免责声明

本产品仅用于实验研究，不得作为药物使用，不得用于家用或其它用途。

l  参考文献

1.    http://www.drugbank.ca

2.    https://ncit.nci.nih.gov

3.    https://www.ncbi.nlm.nih.gov