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GS967

Name: GS967
Brand: TargetMol
SKU: T2049
Price: 30 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T2049Cas No. 1262618-39-2

Alias GS458967

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

GS967

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Purity: 99.63%

Catalog No. T2049Alias GS458967Cas No. 1262618-39-2

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

Pack Size	Price	USA Warehouse	Global Warehouse
2 mg	$30	In Stock	In Stock
5 mg	$48	In Stock	In Stock
10 mg	$72	In Stock	In Stock
25 mg	$162	In Stock	In Stock
50 mg	$298	In Stock	In Stock
100 mg	$522	In Stock	In Stock
200 mg	$756	In Stock	In Stock
500 mg	$1,170	-	In Stock
1 mL x 10 mM (in DMSO)	$53	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Purity:99.63%

Color:White to Yellow

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COA LCMS HNMR

Product Introduction

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.
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

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

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor 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