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GS967

GS967 是一种有效的、选择性的心脏晚期钠电流（late I Na）抑制剂，心室肌细胞和心脏中的IC50分别为0.13和0.21 μM。

CAS号

1262618-39-2

分子式

C14H7F6N3O

主要靶点

Sodium Channel

仅限科研使用

Cat No : CM06492

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Synonyms

GS458967

验证数据展示

  • CAS No.: 1262618-39-2

    GS967
    CAS#: 1262618-39-2

产品信息

GS967 is a potent, and selective inhibitor of cardiac late sodium current (late INa ).

CAS号 1262618-39-2
分子式 C14H7F6N3O
主要靶点 Sodium Channel
主要通路 离子通道
分子量 347.22
纯度 100.00%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名 GS458967

靶点活性

late INa:0.13 μM

体内活性

GS967 prevents and reverses proarrhythmic effects of the late INa enhancer ATX-II and the IKr inhibitor E-4031. GS967 significantly attenuates the proarrhythmic effects of methoxamine 1 clofilium and suppressed ischemia-induced arrhythmias[1]. GS967 causes a reduction of INaP in a frequency-dependent manner, consistent with use-dependent block (UDB). GS967 evokes more potent UDB of INaP (IC50=0.07 μM) than ranolazine (16 μM) and lidocaine (17 μM). GS967 is found to exert these same effects on a prototypical long QT syndromemutation (delKPQ)[2]. GS967 prevents ischemia-induced increases in alternans in the left atrium and left ventricle. GS967 reduces ischemia-induced increases in depolarization heterogeneity and repolarizationheterogeneity. GS967 does not alter heart rate, arterial blood pressure, PR and QT intervals, or QRS duration, but it mildly decreased contractility during ischemia, which was consistent with late INa inhibition[3].

体外活性

GS967 (10, 100, 300 nM) completely attenuates the effect of ATX-II (10 nM) to increase action potential duration (APD) and APD variability in ventricular myocytes, with an apparent IC50 value of ～10 nM and decreased the beat-to-beat variability of APD[1].

溶解度

DMSO:50 mg/mL (144 mM)

参考文献

1.Belardinelli L, et al. A novel, potent, and selective inhibitor of cardiac late sodium current suppresses experimental arrhythmias. J Pharmacol Exp Ther. 2013 Jan;344(1):23-32.
2.Potet F, et al. Use-Dependent Block of Human Cardiac Sodium Channels by GS967. Mol Pharmacol. 2016 Jul;90(1):52-60.
3.Bonatti R, et al. Selective late sodium current blockade with GS-458967 markedly reduces ischemia-induced atrial and ventricular repolarization alternans and ECG heterogeneity. Heart Rhythm. 2014 Oct;11(10):1827-35.

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