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GS967inhibitor of cardiac late sodium current

GS967

Catalog No. B5850
Size Price Stock Qty
10mM (in 1mL DMSO) $110.00 In stock
5mg $100.00 In stock
10mg $150.00 In stock
50mg $450.00 In stock
100mg $640.00 In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

GS967

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Chemical Properties

Cas No. 1262618-39-2 SDF Download SDF
Chemical Name 6-(4-(trifluoromethoxy)phenyl)-3-(trifluoromethyl)-[1,2,4]triazolo[4,3-a]pyridine
Canonical SMILES FC(F)(F)C1=NN=C2C=CC(C3=CC=C(OC(F)(F)F)C=C3)=CN21
Formula C14H7F6N3O M.Wt 347.22
Solubility >13.35mg/mL in DMSO Storage Store at -20°C
General tips N/A
Shipping Condition N/A

Background

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]

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