GS967

GS967 (GS-458967) is a potent, and selective inhibitor of cardiac late sodium current (late INa) with IC50 values of 0.13 and 0.21 μM for ventricular myocytes and isolated hearts, respectively.

Product Specifications

CAS Number

[1262618-39-2]

UNSPSC

12352005

Hazard Statement

H302, H315, H320, H335

Target

Sodium Channel

Type

Reference compound

Related Pathways

Membrane Transporter/Ion Channel

Applications

COVID-19-immunoregulation

Field of Research

Cardiovascular Disease

Assay Protocol

https://www.medchemexpress.com/GS967.html

Concentration

10mM

Purity

99.55

Solubility

DMSO : 50 mg/mL (ultrasonic)

Smiles

FC(C1=NN=C2C=CC(C3=CC=C(OC(F)(F)F)C=C3)=CN21)(F)F

Molecular Formula

C14H7F6N3O

Molecular Weight

347.22

Precautions

H302, H315, H320, H335

References & Citations

[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.|[4]Wei X, et al. Pre- and Delayed Treatments With Ranolazine Ameliorate Ventricular Arrhythmias and Nav1.5 Downregulation in Ischemic/Reperfused Rat Hearts. J Cardiovasc Pharmacol. 2016 Oct;68 (4) :269-279.