GS967
- CAS NO.:1262618-39-2
- Empirical Formula: C14H7F6N3O
- Molecular Weight: 347.22
- MDL number: MFCD28385879
- SAFETY DATA SHEET (SDS)
- Update Date: 2024-07-02 08:55:16
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)-tert-butyl (4-methyl-1-oxopentan-3-yl)carbamate (2S,4R)-4-amino-2-methyl-5-phenylpentanoic acid hydrochloride Tubulysin B Tubulysin H 2,2-diethoxyethanethioamide 2,2-Difluoropropylamine hydrochloride Isoxazole, 3-[[[5-(difluoromethoxy)-1-methyl-3-(trifluoromethyl)-1H-pyrazol-4-yl]methyl]thio]-4,5-dihydro-5,5-dimethyl- 2,2-Difluoropropanol 3-METHYLAZETIDIN-3-OL HYDROCHLORIDE CYCLOBUTYLAMINE HYDROCHLORIDE 4,4-DIFLUOROPIPERIDINE Calcium Sodium Phosphosilicate IH 2-(1-(Mercaptomethyl) cyclopropyl) acetonitrile Fuel shell 2-[2-[3(S)-3[2-(7-chloro-2-quinolinyl) ethenyl] phenyl-3- hydroxyl propyl] phenyl]-2-propanol (1R,2S)-2-(3,4-Difluorophenyl)cyclopropanamine 2-[[(3aR,4S,6R,6aS)-6-Aminotetrahydro-2,2-dimethyl-4H-cyclopenta-1,3-dioxol-4-yl]oxy]ethanol ethanedioate Magnesium Trisilicate Latanoprostene Bunod Lubiprostone Flame Retardant Zinc Borate methyl 3-fluoro-4- thiomorpholino phenylcarbamate (R)-(3-(3-fluoro-4- thiomorpholinophenyl)-2- oxooxazolidin-4-yl) methyl methanesulfonate 1H-Imidazole-4-carbonitrileRelated products of tetrahydrofuran
You may like
-
(R)-(3-(3-fluoro-4- thiomorpholinophenyl)-2- oxooxazolidin-4-yl) methyl methanesulfonateView Details
2416850-45-6 -
methyl 3-fluoro-4- thiomorpholino phenylcarbamateView Details
2760359-22-4 -
Fuel shell 98%View Details
-
4,6-dichloro-2-propylthiopyrimidine-5-amine 145783-15-9 98%View Details
145783-15-9 -
Hydrogen Gas 98%View Details
-
151767-02-1 Montelukast Sodium IP/USP 98%View Details
151767-02-1 -
Valacyclovir Hydrochloride IH 98%View Details
124832-27-5 -
2-[2-[3(S)-3[2-(7-chloro-2-quinolinyl) ethenyl] phenyl-3- hydroxyl propyl] phenyl]-2-propanol 98%View Details
142569-70-8