化合物GS967 T2049

Product Introduction
Bioactivity


英文名: GS967

描述: 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。

激酶实验: The IC50 of LY-364947 at different enzyme concentrations are determined by the filter-binding assay. Typically, 40 μL reactions in 50 mM HEPES at pH 7.5, 1 mM NaF, 200 μM pKSmad3(-3), and 50 mM ATP containing a titration of each inhibitor with concentrations of 1600, 800, 400, 200, 100, 50, 25, and 0 nM are incubated at 30°C for 30 min. The IC50 is calculated using a nonlinear regression method with GraphPad Prism software. The binding type is determined by plotting the correlation between enzyme concentrations and IC50 values.

体外活性: GS967（10、100、300纳摩尔）完全抑制了ATX-II（10纳摩尔）增加心室肌细胞动作电位持续时间（APD）及APD变异性的效果，表观IC50值约为10纳摩尔，且减少了APD的搏动间变异性[1]。

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].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 50 mg/mL (144 mM)


关键字: GS 967 | inhibit | GS 458967 | Na+ channels | GS-967 | Na channels | GS-458967 | GS967 | Sodium Channel | Inhibitor

相关产品: DS-1971a | Zonisamide | 11Beta-hydroxyprogesterone | Rilmakalim | µ-Conotoxin-CnIIIC | Levobupivacaine hydrochloride | Jingzhaotoxin XI | Ropivacaine hydrochloride monohydrate | Rufinamide | GX-674

相关库: Ion Channel Inhibitor Library | ReFRAME Related Library | Anti-Cancer Compound Library | Membrane Protein-targeted Compound Library | Bioactive Compounds Library Max | Fluorochemical Library | Inhibitor Library | Sodium Channel Blocker Library | Anti-Cardiovascular Disease Compound Library | NO PAINS Compound Library

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