GS967 (GS458967) is a potent and selective inhibitor of late INa with anti-arrhythmic actions.
Storage Temp
Store at -20°C
Shipped In
Ice chest + Ice pads
Grade
Moligand™
Action Type
INHIBITOR
Mechanism of action
Inhibitor of Na v1.5
Product Description
Information
GS967 GS967 (GS458967) is a potent and selective inhibitor of late I Na with anti-arrhythmic actions.
Targets
late INa 0.13 μM
In vitro
GS967 (3 μM) has no significant effect on L- or T-type calcium channel currents or Na+-Ca2+ exchanger current (INCX), and 1 μM GS967 has minimal or no effect on the ATP-inhibited K+ current or on human cardiac ion channels expressed in human embryonic kidney 293 or Chinese hamster ovary cells. GS967 is a novel sodium channel modulatorspecifically developed to inhibit persistent sodium current, with a 42-fold preference for persistent as opposed to peakcurrent inhibition.
In vivo
GS967 protects against seizures and prematurelethality in vivo. Chronic GS967 does not cause overt behavioraltoxicity or sedation in wild-type mice at theeffective anticonvulsant dose. GS967 suppresses arrhythmogenicity evoked by ischemia, hypokalemia, and catecholamines in canine and porcine models.
Product Properties
ALogP
5.307
Rotatable Bond
4
Associated Targets
SCN2ATclin Sodium channel protein type 2 subunit alpha 0 Activities
1.Koltun DO, Parkhill EQ, Elzein E, Kobayashi T, Notte GT, Kalla R, Jiang RH, Li X, Perry TD, Avila B et al.. (2016) Discovery of triazolopyridine GS-458967, a late sodium current inhibitor (Late INai) of the cardiac NaV 1.5 channel with improved efficacy and potency relative to ranolazine.. Bioorg Med Chem Lett, 26 (13):(3202-3206). [PMID:27080178]
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F2229359