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GSK2982772

Basic information Safety Supplier Related

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
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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.
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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

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