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GS967

Cat. No. M8911
GS967 Structure
Synonym:

GS-458967

Size Price Availability Quantity
10mg USD 200 In stock
50mg USD 700 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

GS967 (GS-458967) is a highly selective late sodium channel current blocker.

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.

In vivo: 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). GS967 prevents ischemia-induced increases in alternans in the left atrium and left ventricle. GS967 reduces ischemia-induced increases in depolarization heterogeneity and repolarizationheterogeneity.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 347.22
Formula C14H7F6N3O
CAS Number 1262618-39-2
Purity >98%
Solubility DMSO 40 mg/mL
Ethanol 40 mg/mL
Storage at -20°C
References

Use-Dependent Block of Human Cardiac Sodium Channels by GS967.
Potet F, et al. Mol Pharmacol. 2016 Jul;90(1):52-60. PMID: 27136942.

Selective late sodium current blockade with GS-458967 markedly reduces ischemia-induced atrial and ventricular repolarization alternans and ECG heterogeneity.
Bonatti R, et al. Heart Rhythm. 2014 Oct;11(10):1827-35. PMID: 24953379.

A novel, potent, and selective inhibitor of cardiac late sodium current suppresses experimental arrhythmias.
Belardinelli L, et al. J Pharmacol Exp Ther. 2013 Jan;344(1):23-32. PMID: 23010360.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: GS967, GS-458967 supplier, Sodium Channel, inhibitors

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