Basic information Safety Supplier Related

GS967

Basic information Safety Supplier Related

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
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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
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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.

GS967Supplier

Shanghai Boyle Chemical Co., Ltd.
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Haoyuan Chemexpress Co., Ltd.
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021-58950125
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AdooQ Bioscience CHINA
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025-58849295 18951903616;
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Shanghai JiYi Biotechnology Co. Ltd.
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13621943973
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LETOPHARM LIMITED
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+86-21-5821 5861
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