GS967 (GS-458967)是有效地选择性的心脏晚期钠电流抑制剂（late I_Na），在心室肌细胞和心脏中的IC₅₀值分别为0.13和0.21 μM。

GS967 (GS-458967) is a potent, and selective inhibitor of cardiac late sodium current (late I Na ) with IC 50 values of 0.13 and 0.21 μM for ventricular myocytes and isolated hearts, respectively.

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IC50: 0.13 μM (late INa , ventricular myocytes )and 0.21 μM (late INa , isolated hearts)

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. has not independently confirmed the accuracy of these methods. They are for reference only.

GS967 prevents and reverses proarrhythmic effects of the late I Na enhancer ATX-II and the I Kr inhibitor E-4031. GS967 significantly attenuates the proarrhythmic effects of methoxamine 1 clofilium and suppressed ischemia-induced arrhythmias. GS967 causes a reduction of I NaP in a frequency-dependent manner, consistent with use-dependent block (UDB). GS967 evokes more potent UDB of I NaP (IC 50 =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). 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 dur

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[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]. Wei X, et al. Pre- and Delayed Treatments With Ranolazine Ameliorate Ventricular Arrhythmias and Nav1.5 Downregulation in Ischemic/Reperfused Rat Hearts. J Cardiovasc Pharmacol. 2016 Oct;68(4):269-279.

In Vitro: DMSO : 50 mg/mL (144.00 mM; Need ultrasonic)配制储备液