Selonsertib
- Product Name
- Selonsertib
- CAS No.
- 1448428-04-3
- Chemical Name
- Selonsertib
- Synonyms
- GS 4997;CS-2217;GS-4497;Selonsertib;GS-4997;ASK-1;GS4997;GS 4997;GS4997 SELONSERTIB;Selonsertib GS-4997;Selonsertib free base.;Selonsertib (Synonyms: GS-4997)
- CBNumber
- CB03122039
- Molecular Formula
- C24H24FN7O
- Formula Weight
- 445.49
- MOL File
- 1448428-04-3.mol
Selonsertib Property
- 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
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H373May cause damage to organs through prolonged or repeated exposure
- Precautionary statements
-
P260Do not breathe dust/fume/gas/mist/vapours/spray.
P314Get medical advice/attention if you feel unwell.
P501Dispose of contents/container to..…
N-Bromosuccinimide Price
- Product number
- 20972
- Product name
- Selonsertib
- Purity
- ≥95%
- Packaging
- 500μg
- Price
- $32
- Updated
- 2024/03/01
- Product number
- 20972
- Product name
- Selonsertib
- Purity
- ≥95%
- Packaging
- 1mg
- Price
- $57
- Updated
- 2024/03/01
- Product number
- 20972
- Product name
- Selonsertib
- Purity
- ≥95%
- Packaging
- 5mg
- Price
- $214
- Updated
- 2024/03/01
- Product number
- 20972
- Product name
- Selonsertib
- Purity
- ≥95%
- Packaging
- 10mg
- Price
- $335
- Updated
- 2024/03/01
- Product number
- S253800
- Product name
- Selonsertib
- Packaging
- 10mg
- Price
- $315
- Updated
- 2021/12/16
Selonsertib Chemical Properties,Usage,Production
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
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View Lastest Price from Selonsertib manufacturers
- Product
- Selonsertib 1448428-04-3
- Price
- US $9.80/KG
- Min. Order
- 1g
- Purity
- ≥99%
- Supply Ability
- 100kg
- Release date
- 2019-12-21
- Product
- Selonsertib 1448428-04-3
- Price
- US $10.00/KG/Tin
- Min. Order
- 1KG/Tin
- Purity
- 99%
- Supply Ability
- 100
- Release date
- 2019-06-21