GS967

SKU: orb1306639

Description

GS967 is a selective small molecule inhibitor of the cardiac late sodium current (late INa). It is a valuable research tool for investigating cardiac arrhythmias, ischemia-reperfusion injury, and heart failure in both in vitro and in vivo experimental models.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 1262618-39-2
• MW: 347.22
• Purity: >99.99% (May vary between batches)
• Formula: C₁₄H₇F₆N₃O
• SMILES: FC(F)(F)Oc1ccc(cc1)-c1ccc2nnc(n2c1)C(F)(F)F
• Target: Sodium Channel
• Solubility: DMSO:50 mg/mL (144 mM);10% DMSO+90% Corn Oil:2.5 mg/mL (7.2 mM)

Bioactivity

• Target IC50:
  Late INa:0.13 μM
• 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.
• 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.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Na+ channels, Na channels, inhibit, late INa ,isolated hearts, late INa ,ventricular myocytes, Inhibitor, GS 967, GS 458967, GS967, GS-967, GS458967, GS-458967, Sodium Channel, SodiumChannel

Compound Identifiers

PubChem CID

58118983