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GS967

Catalog No. T2049 CAS 1262618-39-2

Synonyms: GS458967

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

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GS967, CAS 1262618-39-2

Pack Size	Availability	Price/USD
2 mg	In stock	$ 30.00
5 mg	In stock	$ 48.00
10 mg	In stock	$ 72.00
25 mg	In stock	$ 162.00
50 mg	In stock	$ 298.00
100 mg	In stock	$ 522.00
200 mg	In stock	$ 756.00
500 mg	In stock	$ 1,170.00
1 mL * 10 mM (in DMSO)	In stock	$ 53.00

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Purity: 100%

Purity: 99.62%

Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

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.

Synonyms	GS458967
Molecular Weight	347.22
Formula	C14H7F6N3O
CAS No.	1262618-39-2

Storage

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

Solubility Information

DMSO: 50 mg/mL (144 mM)

References and Literature

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.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library ReFRAME Related Library Ion Channel Inhibitor Library Anti-Cancer Compound Library Fluorochemical Library Sodium Channel Blocker Library Bioactive Compound Library Anti-Cardiovascular Disease Compound Library Bioactive Compounds Library Max Preclinical Compound Library

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Keywords

GS967 1262618-39-2 Membrane transporter/Ion channel Sodium Channel GS 967 inhibit GS 458967 GS458967 Na+ channels GS-967 Na channels GS-458967 Inhibitor inhibitor

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