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GS967

Catalog No. T2049Cas No. 1262618-39-2
Alias GS458967

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

GS967

GS967

Purity: 100%
Catalog No. T2049Alias GS458967Cas No. 1262618-39-2
GS967 is a potent, and selective inhibitor of cardiac late sodium current (late INa ).
Pack SizePriceAvailabilityQuantity
2 mg$30In Stock
5 mg$48In Stock
10 mg$72In Stock
25 mg$162In Stock
50 mg$298In Stock
100 mg$522In Stock
200 mg$756In Stock
500 mg$1,170In Stock
1 mL x 10 mM (in DMSO)$53In Stock
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Purity:100%
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Product Introduction

Bioactivity
Description
GS967 is a potent, and selective inhibitor of cardiac late sodium current (late INa ).
Targets&IC50
Late INa:0.13 μM
In vitro
GS967 at concentrations of 10, 100, and 300 nM fully counteracts ATX-II's (10 nM) ability to prolong and vary the action potential duration (APD) in ventricular myocytes. It demonstrates an approximate IC50 value of ~10 nM and reduces the beat-to-beat variability of APD[1].
In vivo
GS967 effectively mitigates and reverses the proarrhythmic consequences induced by the late INa enhancer ATX-II, the IKr inhibitor E-4031, as well as methoxamine, 1 clofilium, and ischemia-induced arrhythmias. It significantly reduces the proarrhythmic effects of these agents and suppresses ischemia-induced arrhythmias. Additionally, GS967 decreases INaP in a frequency-dependent manner, showcasing a use-dependent block (UDB) that is more potent than that of ranolazine and lidocaine, with an IC50 of 0.07 μM compared to 16 μM and 17 μM respectively. This compound also maintains its effectiveness against a common long QT syndrome mutation (delKPQ) and prevents ischemia-induced alternans in both the left atrium and ventricle, alongside reducing depolarization and repolarization heterogeneity induced by ischemia. Notably, GS967 does not affect heart rate, arterial blood pressure, PR and QT intervals, or QRS duration, although it slightly reduces contractility during ischemia, aligning with late INa inhibition effects.
Kinase Assay
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.
AliasGS458967
Chemical Properties
Molecular Weight347.22
FormulaC14H7F6N3O
Cas No.1262618-39-2
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 50 mg/mL (144 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.8800 mL14.4001 mL28.8002 mL144.0009 mL
5 mM0.5760 mL2.8800 mL5.7600 mL28.8002 mL
10 mM0.2880 mL1.4400 mL2.8800 mL14.4001 mL
20 mM0.1440 mL0.7200 mL1.4400 mL7.2000 mL
50 mM0.0576 mL0.2880 mL0.5760 mL2.8800 mL
100 mM0.0288 mL0.1440 mL0.2880 mL1.4400 mL

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