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GS967 Sodium Channel inhibitor

Cat.No.S5274

GS967 (GS458967) is a potent and selective inhibitor of late INa with anti-arrhythmic actions.
GS967 Sodium Channel inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 347.22

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: S527401 Ethanol]46 mg/mL]false]DMSO]45 mg/mL]false]Water]Insoluble]false Purity: 99.98%
99.98

Chemical Information, Storage & Stability

Molecular Weight 347.22 Formula

C14H7F6N3O

 Storage (From the date of receipt)
CAS No. 1262618-39-2 -- Storage of Stock Solutions

Synonyms GS458967 Smiles C1=CC(=CC=C1C2=CN3C(=NN=C3C(F)(F)F)C=C2)OC(F)(F)F

Solubility

In vitro
Batch:

Ethanol : 46 mg/mL

DMSO : 45 mg/mL (129.6 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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mg/kg g μL

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% DMSO % % Tween 80 % ddH2O
%DMSO %

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC50/Ki
late INa [1]
0.13 μM
In vitro
GS967 (3 μM) has no significant effect on L- or T-type calcium channel currents or Na+-Ca2+ exchanger current (INCX), and 1 μM of this compound has minimal or no effect on the ATP-inhibited K+ current or on human cardiac ion channels expressed in human embryonic kidney 293 or Chinese hamster ovary cells[1]. This compound is a novel sodium channel modulator specifically developed to inhibit persistent sodium current, with a 42-fold preference for persistent as opposed to peak current inhibition[2].
In vivo
GS967 protects against seizures and premature lethality in vivo. Chronic administration of this compound does not cause overt behavioral toxicity or sedation in wild-type mice at the effective anticonvulsant dose[2]. It suppresses arrhythmogenicity evoked by ischemia, hypokalemia, and catecholamines in canine and porcine models[3].
References

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