Powder: -20°C for 3 years | In solvent: -80°C for 1 year
GS967 is a potent, and selective inhibitor of cardiac late sodium current (late INa ).
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
2 mg | In stock | $ 30.00 | |
5 mg | In stock | $ 48.00 | |
10 mg | In stock | $ 72.00 | |
25 mg | In stock | $ 162.00 | |
50 mg | In stock | $ 298.00 | |
100 mg | In stock | $ 522.00 | |
200 mg | In stock | $ 756.00 | |
500 mg | In stock | $ 1,170.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 53.00 |
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 (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]. |
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 |
Molecular Weight | 347.22 |
Formula | C14H7F6N3O |
CAS No. | 1262618-39-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 50 mg/mL (144 mM)
You can also refer to dose conversion for different animals. More
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GS967 1262618-39-2 Membrane transporter/Ion channel Sodium Channel GS 967 inhibit GS 458967 GS458967 Na+ channels GS-967 Na channels GS-458967 Inhibitor inhibitor