1. Membrane Transporter/Ion Channel
  2. Sodium Channel
  3. GS967

GS967 

Cat. No.: HY-12593 Purity: 99.96%
Handling Instructions

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.

For research use only. We do not sell to patients.

GS967 Chemical Structure

GS967 Chemical Structure

CAS No. : 1262618-39-2

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 132 In-stock
Estimated Time of Arrival: December 31
5 mg USD 120 In-stock
Estimated Time of Arrival: December 31
10 mg USD 180 In-stock
Estimated Time of Arrival: December 31
50 mg USD 540 In-stock
Estimated Time of Arrival: December 31
100 mg USD 768 In-stock
Estimated Time of Arrival: December 31
200 mg USD 1128 In-stock
Estimated Time of Arrival: December 31
500 mg   Get quote  
1 g   Get quote  

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Top Publications Citing Use of Products

    GS967 purchased from MCE. Usage Cited in: Circ Arrhythm Electrophysiol. 2017 Mar;10(3). pii: e004331.

    Effects of ranolazine and GS-967 on susceptibility to induction of ventricular refibrillation and spontaneous termination of initial long duration ventricular fibrillation (LDVF).

    GS967 purchased from MCE. Usage Cited in: J Cardiovasc Pharmacol. 2016 Oct;68(4):269-279.

    Expression of total Nav1.5 protein is determined by Western blotting and the intensity of the bands is quantified by densitometry.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    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.

    IC50 & Target

    IC50: 0.13 μM (late INa , ventricular myocytes )and 0.21 μM (late INa , isolated hearts)[1]

    In Vitro

    GS967 (10, 100, 300 nM) completely attenuates the effect of ATX-II (10 nM) to increase action potential duration (APD) and APD variability in ventricular myocytes, with an apparent IC50 value of ∼10 nM and decreased the beat-to-beat variability of APD[1].

    In Vivo

    GS967 prevents and reverses proarrhythmic effects of the late INa enhancer ATX-II and the IKr inhibitor E-4031. GS967 significantly attenuates the proarrhythmic effects of methoxamine 1 clofilium and suppressed ischemia-induced arrhythmias[1]. GS967 causes a reduction of INaP in a frequency-dependent manner, consistent with use-dependent block (UDB). GS967 evokes more potent UDB of INaP (IC50=0.07 μM) than ranolazine (16 μM) and lidocaine (17 μM). GS967 is found to exert these same effects on a prototypical long QT syndromemutation (delKPQ)[2]. GS967 prevents ischemia-induced increases in alternans in the left atrium and left ventricle. GS967 reduces ischemia-induced increases in depolarization heterogeneity and repolarizationheterogeneity. GS967 does not alter heart rate, arterial blood pressure, PR and QT intervals, or QRS duration, but it mildly decreased contractility during ischemia, which was consistent with late INa inhibition[3].

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 50 mg/mL (144.00 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.8800 mL 14.4001 mL 28.8002 mL
    5 mM 0.5760 mL 2.8800 mL 5.7600 mL
    10 mM 0.2880 mL 1.4400 mL 2.8800 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (7.20 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: 2.5 mg/mL (7.20 mM); Suspended solution; Need ultrasonic

    *All of the co-solvents are provided by MCE.
    References
    Animal Administration
    [1][2]

    Rats: Ventricular tachycardia or fibrillation are induced either by local aconitine injection (50 μg) in the left ventricular muscle of adult male rats or by arterial perfusion of 0.1 mM hydrogen peroxide in aged male rats. The left ventricular epicardial surface of the isolated-perfused hearts is optically mapped using fluorescent voltage-sensitive dye, and microelectrode recordings of action potentials are made adjacent to the aconitine injection site. The suppressive and preventive effects of GS967 (1 μM) against EAD/DAD-mediated ventricular tachycardia or fibrillation are then determined[2].

    Rabbits: To determine the effect of GS967 on the inducibility of TdP by clofilium in the presence of methoxamine, rabbits are first treated with either vehicle or GS967 (in randomized manner) given as a 60 μg/kg bolus, followed by a 16 μg/kg/min infusion that is maintained for the duration of an experiment. After 10 minutes, methoxamine is infused intravenously at 15 μg/kg/min, followed 10 minutes later by clofilium at 100 nmol/kg/min. The incidences of premature ventricular contractions (PVCs), ventricular tachycardia (VT; defined as three or more consecutive abnormal beats), and TdP are determined from the ECG recordings[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
    Molecular Weight

    347.22

    Formula

    C₁₄H₇F₆N₃O

    CAS No.

    1262618-39-2

    SMILES

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

    Shipping

    Room temperature in continental US; may vary elsewhere

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    This equation is commonly abbreviated as: C1V1 = C2V2

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    Product Name:
    GS967
    Cat. No.:
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    GS967

    Cat. No.: HY-12593