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GS967 [1262618-39-2]

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Cat# T2049-5mg

Size : 5mg

Brand : TargetMol

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GS967

(Synonyms: GS458967) Copy Product Info

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

Cas No. 1262618-39-2

With extensive experience in compound synthesis, we can provide rapid custom synthesis services for this product according to your research needs.

For research use only—not for human use. No sales to individuals. Use as intended only.

Batch Information

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Purity:99.63%

Color:White to Yellow

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COA HNMR LCMS

Product Information

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.
Synonyms	GS458967
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.

Chemical Properties

Molecular Weight	347.22
Formula	C₁₄H₇F₆N₃O
Cas No.	1262618-39-2
Smiles	FC(F)(F)Oc1ccc(cc1)-c1ccc2nnc(n2c1)C(F)(F)F
Relative Density.	1.52 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 50 mg/mL (144 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+90% Corn Oil: 2.5 mg/mL (7.2 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.8800 mL	14.4001 mL	28.8002 mL	144.0009 mL
5 mM	0.5760 mL	2.8800 mL	5.7600 mL	28.8002 mL
10 mM	0.2880 mL	1.4400 mL	2.8800 mL	14.4001 mL
20 mM	0.1440 mL	0.7200 mL	1.4400 mL	7.2000 mL
50 mM	0.0576 mL	0.2880 mL	0.5760 mL	2.8800 mL
100 mM	0.0288 mL	0.1440 mL	0.2880 mL	1.4400 mL

Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

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Tech Support

Please see Product Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc