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Selonsertib(GS-4997)

Names

[ CAS No. ]:
1448428-04-3

[ Name ]:
Selonsertib(GS-4997)

[Synonym ]:
selonsertib
Benzamide, 5-(4-cyclopropyl-1H-imidazol-1-yl)-2-fluoro-4-methyl-N-[6-[4-(1-methylethyl)-4H-1,2,4-triazol-3-yl]-2-pyridinyl]-
UNII:NS3988A2TC
5-(4-Cyclopropyl-1H-imidazol-1-yl)-2-fluoro-N-[6-(4-isopropyl-4H-1,2,4-triazol-3-yl)-2-pyridinyl]-4-methylbenzamide
GS-4997

Biological Activity

[Description]:

Selonsertib is an apoptosis signal-regulating kinase 1 (ASK1) inhibitor with a pIC50 of 8.3±0.07.

[Related Catalog]:

Signaling Pathways >> MAPK/ERK Pathway >> MAP3K
Research Areas >> Cancer

[Target]

ASK1:8.3 (pIC50)


[In Vitro]

Selonsertib (GS-4997) is a clinical stage ASK1 inhibitor, which has been evaluated as an experimental treatment for diabetic nephropathy and kidney fibrosis[1]. Selonsertib (GS-4997) is a highly selective and potent once-daily oral ASK1 inhibitor that competes with ATP in the ASK1 catalytic kinase domain[2].

[References]

[1]. Lanier M, et al. Structure-Based Design of ASK1 Inhibitors as Potential Agents for Heart Failure. ACS Med Chem Lett. 2017 Feb 8;8(3):316-320.

[2]. Lin JH, et al. Design of a phase 2 clinical trial of an ASK1 inhibitor, GS-4997, in patients with diabetic kidney disease. Nephron. 2015;129(1):29-33.


[Related Small Molecules]

Takinib | NG25 | GNE-3511 | 5Z-7-Oxozeaenol | NQDI 1 | GS-444217 | B-Raf inhibitor

Chemical & Physical Properties

[ Density]:
1.4±0.1 g/cm3

[ Molecular Formula ]:
C24H24FN7O

[ Molecular Weight ]:
445.492

[ Exact Mass ]:
445.202637

[ LogP ]:
3.17

[ Index of Refraction ]:
1.704

[ Storage condition ]:
-20℃

Related Compounds