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CAS No.: 1262618-39-2

GS967 Catalog No. CSN16320

Synonyms: GS458967

GS-967 is a selective inhibitor of cardiac late sodium current (late INa ). The IC50 values in ventricular myocytes and isolated hearts are 0.13 μM and 0.21 μM.

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技术信息

生物活性

描述GS-967 is a selective inhibitor of cardiac late sodium current (late INa ). The IC50 values in ventricular myocytes and isolated hearts are 0.13 μM and 0.21 μM. Selective inhibition of the INa-L (late Na) without affecting their peak transients with the highly specific prototype drug, GS-967 suppresses these EAD (early afterdepolarizations)-mediated VT/VFs^[3]. GS967 (IC50 ~200nM) significantly shortened repolarization in canine ventricular cardiomyocytes and sinus rhythm (SR) dogs, in a concentration and dose-dependent manner. In vitro, despite addition of 1μM GS967, dofetilide-induced EADs remained present in 42% and 35% of cardiomyocytes from SR (sinus rhythm) and CAVB (chronic atrioventricular block) dogs, respectively. The antiarrhythmic mode of action of GS967, through the reduction of spatial dispersion of repolarization, seems to predominantly impede the perpetuation of arrhythmic events into TdP (Torsades de Pointes arrhythmias) rather than their initiating trigger^[4]. GS-967 reduced septal myocardium tension during simulated exercise in vitro and therefore have the potential to ameliorate symptoms caused by inducible obstruction in HCM (hypertrophic cardiomyopathy) patients^[5]. Chronic treatment with GS-967 dose-dependently reduced LV mass, the increases in E/E' (early transmitral flow velocity/early mitral annulus velocity) ratio, and the prolongation of IVRT (isovolumic relaxation time) by 27, 27, and 20%, respectively, at the 1.0 mg·kg(-1)·day(-1) dose without affecting blood pressure or LV (left ventricular) systolic function. The prolonged APDs (action potential duration) in myocytes and QTc of HS (high-salt) rats were significantly reduced with GS-967 treatment^[6].
参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.8801 mL
- 14.4003 mL
- 28.8006 mL
- 5 mM
- 0.5760 mL
- 2.8801 mL
- 5.7601 mL
- 10 mM
- 0.2880 mL
- 1.4400 mL
- 2.8801 mL

技术信息

CAS号

1262618-39-2

储存条件

粉末: Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C14H7F6N3O

运输

蓝冰

分子量

347.22

别名

GS458967

溶解度

DMSO	62.0 mg/mL (178.6 mM)
Water	insoluble

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