| Identification | Back Directory | [Name]
1,2,4-Triazolo[4,3-a]pyridin-3(2H)-one, 2-[(3-methyl-1,2,4-oxadiazol-5-yl)methyl]-6-[4-(trifluoromethoxy)phenyl]- | [CAS]
1354198-41-6 | [Synonyms]
GS462808
GS-462808
GS 462808
1,2,4-Triazolo[4,3-a]pyridin-3(2H)-one, 2-[(3-methyl-1,2,4-oxadiazol-5-yl)methyl]-6-[4-(trifluoromethoxy)phenyl]- | [Molecular Formula]
C17H12F3N5O3 | [MOL File]
1354198-41-6.mol | [Molecular Weight]
391.3 |
| Hazard Information | Back Directory | [Description]
GS-462808 is a late sodium current inhibitor (Late INai) of the cardiac Nav1.5 channel with improved efficacy and potency relative to ranolazine. GS-462808 had lower brain penetration and serendipitously lower activity at the brain isoforms. GS-462808 has an improved CNS window , and improved anti-ischemic potency relative to ranolazine. | [Uses]
GS-462808 is an oral active late sodium current inhibitor (Late INai) of the cardiac Nav1.5 channel with the IC50 of 1.33 μM. GS-462808 can be used for study of arrhythmia[1]. | [IC 50]
Nav1.5: 1.33 μM (IC50) | [References]
[1] Koltun DO, et al. Discovery of triazolopyridinone GS-462808, a late sodium current inhibitor (Late INai) of the cardiac Nav1.5 channel with improved efficacy and potency relative to ranolazine. Bioorg Med Chem Lett. 2016;26(13):3207-3211. DOI:10.1016/j.bmcl.2016.03.096 |
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