Cas：1448428-04-3 (free base)
Selonsertib, also known as GS-4997, is an orally bioavailable inhibitor of apoptosis signal-regulating kinase 1 (ASK1), with potential anti-inflammatory, antineoplastic and anti-fibrotic activities. GS-4997 targets and binds to the catalytic kinase domain of ASK1 in an ATP-competitive manner, thereby preventing its phosphorylation and activation. GS-4997 prevents the production of inflammatory cytokines, down-regulates the expression of genes involved in fibrosis, suppresses excessive apoptosis and inhibits cellular proliferation.
Chemical Formula: C24H24FN7O
Exact Mass: 445.20264
Molecular Weight: 445.5
Elemental Analysis: C, 64.71; H, 5.43; F, 4.26; N, 22.01; O, 3.59
Selonsertib free base
Chemical Name: 5-(4-cyclopropyl-1H-imidazol-1-yl)-2-fluoro-N-(6-(4-isopropyl-4H-1,2,4-triazol-3-yl)pyridin-2-yl)-4-methylbenzamide
InChi Code: InChI=1S/C24H24FN7O/c1-14(2)32-13-27-30-23(32)19-5-4-6-22(28-19)29-24(33)17-10-21(15(3)9-18(17)25)31-11-20(26-12-31)16-7-8-16/h4-6,9-14,16H,7-8H2,1-3H3,(H,28,29,33)
Appearance: White to off-white
Purity: >98% (Note: HPLC, LC/MS may detect up to ~ 5% tautomer depending on
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >5 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
Selonsertib (GS-4997) is a clinical stage ASK1 inhibitor, which has been evaluated as an experimental treatment for diabetic nephropathy and kidney fibrosis. Selonsertib (GS-4997) is a highly selective and potent once-daily oral ASK1 inhibitor that competes with ATP in the ASK1 catalytic kinase domain.
Ji N, Yang Y, Cai CY, Lei ZN, Wang JQ, Gupta P, Shukla S, Ambudkar SV, Kong D, Chen ZS. Selonsertib (GS-4997), an ASK1 inhibitor, antagonizes multidrug resistance in ABCB1- and ABCG2-overexpressing cancer cells. Cancer Lett. 2019 Jan;440-441:82-93. doi: 10.1016/j.canlet.2018.10.007. Epub 2018 Oct 10. PubMed PMID: 30315846.
Nelson CH, Wang L, Fang L, Weng W, Cheng F, Hepner M, Lin J, Garnett C, Ramanathan S. A Quantitative Framework to Evaluate Proarrhythmic Risk in a First-in-Human Study to Support Waiver of a Thorough QT Study. Clin Pharmacol Ther. 2015 Dec;98(6):630-8. doi: 10.1002/cpt.204. Epub 2015 Sep 29. PubMed PMID: 26259519.
3. Lin JH, Zhang JJ, Lin SL, Chertow GM. 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. doi: 10.1159/000369152. Epub 2014 Dec 17. PubMed PMID: 25531162.
Products are for research use only. Not for human use.
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