Basic information Safety Supplier Related

Selonsertib

Basic information Safety Supplier Related

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
Product Categories:
  • API
Mol File:
1448428-04-3.mol
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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)
pka
11.21±0.70(Predicted)
form 
solid
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.
InChIKey
YIDDLAAKOYYGJG-UHFFFAOYSA-N
SMILES
C(NC1=NC(C2N(C(C)C)C=NN=2)=CC=C1)(=O)C1=CC(N2C=NC(C3CC3)=C2)=C(C)C=C1F
CAS DataBase Reference
1448428-04-3
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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

SelonsertibSupplier

Shanghai Boyle Chemical Co., Ltd.
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WUHAN SUN-SHINE BIO-TECHNOLOGY Co., Ltd.
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17702719238 17702719238
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Dalian Meilun Biotech Co., Ltd.
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0411-62910999 13889544652
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Shanghai Topbiochem Technology Co., Ltd
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021-58170097
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Shanghai Xingui Biotechnology Co., Ltd.
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17501653715
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xingui2022@126.com