Selonsertib Struktur

Selonsertib

Bezeichnung:Selonsertib

CAS-Nr1448428-04-3

Englisch Name:Selonsertib

CBNumberCB03122039

SummenformelC24H24FN7O

Molgewicht445.49

MOL-Datei1448428-04-3.mol

Selonsertib physikalisch-chemischer Eigenschaften

Schmelzpunkt	>180°C (dec.)
Dichte	1.39±0.1 g/cm3(Predicted)
storage temp.	-20°C
Löslichkeit	Soluble in DMSO (>25 mg/ml)
pka	11.21±0.70(Predicted)
Aggregatzustand	solid
Farbe	White
Stabilität	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 Datenbank	1448428-04-3

Gefahreninformationscode (GHS)

Selonsertib Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung
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
Verwenden
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].
Einzelnachweise
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 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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