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MedChemExpressModel Selonsertib - 1448428-04-3

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Selonsertib (GS-4997), an orally bioavailable, selective apoptosis signal-regulating kinase 1 (ASK1) inhibitor with a pIC50 of 8.3, has been evaluated as an experimental treatment for diabetic nephropathy and kidney fibrosis.
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Selonsertib

MCE China:Selonsertib

Brand:MedChemExpress (MCE)

Cat. No.HY-18938

CAS:1448428-04-3

Synonyms:GS-4997

Purity:99.05%

Storage:Powder -20°C 3 years 4°C 2 years In solvent -80°C 1 year -20°C 6 months

Shipping:Room temperature in continental US; may vary elsewhere.

Description:Selonsertib (GS-4997), an orally bioavailable, selective apoptosis signal-regulating kinase 1 (ASK1) inhibitor with a pIC50 of 8.3, has been evaluated as an experimental treatment for diabetic nephropathy and kidney fibrosis.

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].

IC50 & Target:ASK1 8.3 (pIC50)

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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.  [Content Brief]

[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.  [Content Brief]

[3]. Loomba R, et al. The ASK1 inhibitor selonsertib in patients with nonalcoholic steatohepatitis: A randomized, phase 2trial. Hepatology. 2018 Feb;67(2):549-559.  [Content Brief]

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