GS967
GS967 Basic information
- Product Name:
- GS967
- Synonyms:
-
- GS967
- 6-(4-(trifluoroMethoxy)phenyl)-3-(trifluoroMethyl)-[1,2,4]triazolo[4,3-a]pyridine
- GS 458967
- GS458967
- GS-458967
- GS-967;GS 967;GS-458967; GS 458967; GS458967
- GS967(GS-458967)
- GS967, >98%
- CAS:
- 1262618-39-2
- MF:
- C14H7F6N3O
- MW:
- 347.22
- Product Categories:
-
- Inhibitors
- Mol File:
- 1262618-39-2.mol
GS967 Chemical Properties
- 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
GS967 Usage And Synthesis
Uses
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.
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