GSK2982772
GSK2982772 Basic information
- Product Name:
- GSK2982772
- Synonyms:
-
- (S)-5-benzyl-N-(5-methyl-4-oxo-2,3,4,5-tetrahydrobenzo[b][1,4]oxazepin-3-yl)-4H-1,2,4-triazole-3-carboxamide
- 5184
- GSK2982772
- RIP1 inhibitor GS2982772
- CS-2502
- (S)-5-BENZYL-N-(5-METHYL-4-OXO-2,3,4,5-TETRAHYDROBENZO[B][1,4]OXAZEPIN-3-YL)-4H-1,2,4-TRIAZOLE-3-CAR
- GSK 2982772;GSK-2982772
- 1H-1,2,4-Triazole-5-carboxamide, 3-(phenylmethyl)-N-[(3S)-2,3,4,5-tetrahydro-5-methyl-4-oxo-1,5-benzoxazepin-3-yl]-
- CAS:
- 1622848-92-3
- MF:
- C20H19N5O3
- MW:
- 377.4
- Mol File:
- 1622848-92-3.mol
GSK2982772 Chemical Properties
- Density
- 1.40±0.1 g/cm3(Predicted)
- storage temp.
- -20°C
- solubility
- Soluble in DMSO (>25 mg/ml)
- form
- solid
- pka
- 8.80±0.40(Predicted)
- color
- Off-white
- Stability:
- Stable for 2 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 1 month.
GSK2982772 Usage And Synthesis
Description
(S)-5-benzyl-N-(5-methyl-4-oxo-2,3,4,5-tetrahydrobenzo[b][1,4]oxazepin-3-yl)-4H-1,2,4-triazole-3-carboxamide, also known as GSK2982772, is a first-in-class receptor interacting protein 1(RIP1)-kinase specific clinical candidate for the treatment of inflammatory disease. It is an inhibitor of RIP1 that regulates necroptosis and inflammation and may play an important role in contributing to a variety of human pathologies, including immune-mediated inflammatory diseases. It has excellent activity in blocking many TNF-dependent cellular responses. Highlighting its potential as a novel anti-inflammatory agent, the inhibitor was also able to reduce spontaneous production of cytokines from human ulcerative colitis explants.
References
Harris, P. A., et al. "Discovery of a First-in-Class Receptor Interacting Protein 1 (RIP1) Kinase Specific Clinical Candidate (GSK2982772) for the Treatment of Inflammatory Diseases." Journal of Medicinal Chemistry 60.4(2017):1247-1261.
Jeong, Jae Uk, et al. "Synthesis of ( S )-3-amino-benzo[ b ][1,4]oxazepin-4-one via Mitsunobu and S N Ar reaction for a first-in-class RIP1 kinase inhibitor GSK2982772 in clinical trials." Tetrahedron Letters 58.23(2017):2306-2308.
GSK2982772Supplier
- Tel
- 13761310616
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- Tel
- 0519-85788828 13775037613
- sales@chemrenpharm.com
- Tel
- sales@boylechem.com
- Tel
- 18149758185 18149758185
- sales-cpd@caerulumpharma.com
- Tel
- +86-2332782371 +86-18120098618
- sales@adobechem.com
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