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Postion:Product Catalog >Biochemical Engineering>Biochemical Reagents>Agonist Inhibitors>GS967
GS967
  • GS967

GS967 NEW

Price $48 $72 $153
Package 5mg 10mg 25mg
Supply Ability: 10g
Update Time: 2026-05-26

Product Details

Product Name: GS967 CAS No.: 1262618-39-2
Purity: 99.63% Supply Ability: 10g
Release date: 2026/05/26

Product Introduction

Bioactivity

NameGS967
DescriptionGS967 is a potent, and selective inhibitor of cardiac late sodium current (late INa ).
Kinase AssayThe 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.
In vitroGS967 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 vivoGS967 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.
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.
Solubility InformationDMSO : 50 mg/mL (144 mM), Sonication is recommended.
10% DMSO+90% Corn Oil : 2.5 mg/mL (7.2 mM), Sonication is recommended.
KeywordsSodiumChannel | Sodium Channel | Na+ channels | Na channels | late?INa?,ventricular myocytes | late?INa?,isolated hearts | Inhibitor | inhibit | GS-967 | GS967 | GS-458967 | GS 967 | GS 458967
Inhibitors RelatedPhenytoin sodium | Procaine | Ranolazine dihydrochloride | Tetracaine hydrochloride | Lidocaine | Safinamide | Permethrin | Valproic Acid | L-Aspartic aicd sodium | Lidocaine hydrochloride | Mebeverine hydrochloride | Dibucaine
Related Compound LibrariesBioactive Compound Library | Pain-Related Compound Library | Membrane Protein-targeted Compound Library | Sodium Channel Targeted Library | Neuroprotective Compound Library | Inhibitor Library | Anti-Cardiovascular Disease Compound Library | NO PAINS Compound Library | Bioactive Compounds Library Max | Fluorochemical Library | Preclinical Compound Library | Ion Channel Targeted Library

Company Profile Introduction

Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers. TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.

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