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GS967

CAS No. : 1262618-39-2

MCE 站：GS967

产品活性：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。

研究领域：Membrane Transporter/Ion Channel

作用靶点：Sodium Channel

In Vitro: 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.

In Vivo: 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 (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). 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.

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