GS967
- CAS NO.:1262618-39-2
- Empirical Formula: C14H7F6N3O
- Molecular Weight: 347.22
- MDL number: MFCD28385879
- SAFETY DATA SHEET (SDS)
- Update Date: 2024-11-09 21:40:10
What is GS967?
The Uses of GS967
GS967, also known as GS-458967, is a highly selective late sodium channel current blocker. The selective inhibition of late INa with GS967 can exert antiarrhythmic effects by suppressing EAD- and DAD-mediated extrasystolic activity in PFs and PV and SVC sleeve preparations. Selective late INa inhibition with GS967 exerts potent protective effects against ischemia-induced depolarization and repolarization abnormalities in both atria and ventricles.
Biological Activity
gs967 is a potent, selective and novel inhibitor of cardiac late sodium current (late ina) with ic50=0.13 μm in ventricular myocytes and ic50=0.21μm in isolated hearts. [1]when na+ channels in myocytes fail to inactivate after opening, na+ influx continues throughout the ap plateau. the resulting na+ current (ina) is referred to as late ina. its magnitude is increased in many pathologic conditions, such as in the failing and/or ischemic heart, in the heart exposed to oxidative stress, and in hearts of patients with congenital long qt3 syndromes. [1]in rabbit isolated ventricular myocytes, inhibition of peak ina by gs967 is in a concentration- and voltage-dependent manner with minimal use-dependent, it also decreases the na+ and ca2+ overload. in rabbit-isolated heart, gs967 abolishes tdp induced by atx-ii or e-4031. [1]in anesthetized rabbit, gs967 reduces mapd90 but did not alter cardiac conduction time; it also prevents the induction of arrhythmic activity and tdp by clofilium and decreases the incidence of ischemia-induced arrhythmias. [1]
References
1. belardinelli l, liu g, smith-maxwell c et al. a novel, potent, and selective inhibitor ofcardiac late sodium current suppresses experimental arrhythmias. j pharmacol exp ther. 2013 jan;344(1):23-32.
Properties of GS967
Density | 1.52±0.1 g/cm3(Predicted) |
storage temp. | Store at -20°C |
solubility | insoluble in H2O; ≥13.35 mg/mL in DMSO; ≥25.52 mg/mL in EtOH with ultrasonic |
form | solid |
pka | -0.41±0.50(Predicted) |
color | White to off-white |
Safety information for GS967
Computed Descriptors for GS967
New Products
(R)-3-Aminobutanenitrile Hydrochloride 4-Aminotetrahydropyran-4-carbonitrile Hydrochloride 4-AMINO-TETRAHYDRO-PYRAN-4-CARBOXYLIC ACID HCL 4-AMINO-TETRAHYDRO-PYRAN-4-CARBOXYLIC ACID 1,4-Dioxa-8-azaspiro[4.5]decane 5-Bromo-2-nitropyridine SODIUM AAS SOLUTION ZINC AAS SOLUTION BUFFER SOLUTION PH 10.0(BORATE) GOOCH CRUCIBLE SINTERED AQUANIL 5 BERYLLIUM AAS SOLUTION XANTHAN GUM Racecadotril SODIUM VALPROATE Diclofenac Sodium Methylcobalamin (vitamin B12) SODIUM METHYL PARABEN Folic Acid Impurity G Dabigatran Acyl-O2-D-Glucuronide Trifluoroacetic Acid Salt Glycopyrronium Bromide EP Impurity I Eltrombopag N-Oxide Impurity Di-Nitroso Acyclovir Impurity K DLRD N-OxideRelated products of tetrahydrofuran
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