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| Selonsertib Basic information |
| Product Name: | Selonsertib | | Synonyms: | Selonsertib;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]benzamide;GS 4997;Selonsertib GS-4997;GS-4497;GS-4997;ASK-1;GS4997 SELONSERTIB;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 | | CAS: | 1448428-04-3 | | MF: | C24H24FN7O | | MW: | 445.49 | | EINECS: | | Product Categories: | API | | Mol File: | 1448428-04-3.mol |
| Selonsertib Chemical Properties |
| Melting point | >180°C (dec.) | | density | 1.39±0.1 g/cm3(Predicted) | | storage temp. | -20°C | | solubility | Soluble in DMSO (>25 mg/ml) | | form | solid | | pka | 11.21±0.70(Predicted) | | color | White | | Stability: | Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months. | | CAS DataBase Reference | 1448428-04-3 |
| Selonsertib Usage And Synthesis |
| Description | Selonsertib (1448428-04-3) is a potent Apoptosis signal-regulating kinase 1 (ASK1) inhibitor (pIC50 = 8.3)1 found to improve metabolic parameters in nonalcoholic steatohepatitis, reduce hepatic steatosis, inflammation, and fibrosis2-4. Selonsertib suppressed the efflux function of multidrug resistance (MDR) transporters ABCB1 and ABCG2.5 | | Uses | Selonsertib is an apoptosis signal-regulating kinase 1 (ASK1) inhibitor with potential anti-inflammatory, antineoplastic and anti-fibrotic activities. Selonsertib interacts with the catalytic kinase domain of ASK1 and prevents its phosphorylation and activation. As a result, the expression of genes involved in fibrosis, cellular proliferation, and apoptosis are down regulated. | | in vitro | gs-4997 has been identified as a highly selective and potent ask1 inhibitor that competed with atp in the ask1 catalytic kinase domain. moreover, the ask1 inhibition caused by gs-4997 was found to be significantly different in mechanism from bardoxolone methyl. gs- 4997 could also shut down cell signaling involved in pathogenesis, while bardoxolone methyl activated mrna transcription in every cell exposed to drug. in addition, gs-4997 could selectively target affected cells in which the oxidative burden was high [1]. | | References | Lanier et al. (2017), Structure-Based Design of ASK1 Inhibitors as Potential Agents for Heart Failure; ACS Med. Chem. Lett. 8 316
Loomba et al. (2017), The ASK1 inhibitor selonsertib in patients with nonalcoholic steatohepatitis: a randomized, phase 2 trial; Hepatology 67 549
Younossi et al. (2018), Improvement of hepatic fibrosis and patient-reported outcomes in non-alcoholic steatohepatitis treated with selonsertib; Liver Int. 38 1849
Gawrieh and Chalasani (2018), Emerging Treatments for Nonalcoholic Fatty Liver Disease and Nonalcoholic Steatohepatitis; Clin. Liver Dis. 22 189
Ji et al. (2019), Selonsertib (GS-4997), an ASK1 inhibitor, antagonizes multidrug resistance in ABCB1- and ABCG2-overexpressing cancer cells; Cancer Lett. 440-441 82 |
| Selonsertib Preparation Products And Raw materials |
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