- GSK2982772
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- $68.00 / 1mg
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2025-06-12
- CAS:1622848-92-3
- Min. Order:
- Purity: 99.31%
- Supply Ability: 10g
- GSK2982772
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- $1.00 / 1KG
-
2019-09-02
- CAS:1622848-92-3
- Min. Order: 1KG
- Purity: 98%
- Supply Ability: 1lg; 2kg; 5kg; 10kg; 100kg
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| | 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 | | EINECS: | | | Product Categories: | | | 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. | | Uses | GSK2982772 is a potent, orally active and ATP competitive RIP1 kinase inhibitor with IC50 values of 16 nM and 20 nM for human and monkey RIP1, respectively[1]. | | in vivo | GSK2982772 is dosed orally 15 min prior to TNF and shows 68, 80, and 87% protection from temperature loss over 6 h, at doses of 3, 10, and 50 mg/kg, respectively. In the corresponding TNF/zVAD model, GSK2982772 shows 13, 63, and 93% protection from temperature loss over 3 h. GSK2982772 displays a good free fraction in blood in rats (4.2%), dogs (11%), cynomolgus monkeys (11%), and humans (7.4%). The inhibitor has a good pharmacokinetic profile across both rats and monkeys. GSK2982772 distributes into a range of tissues including the colon, liver, kidney, and heart at concentrations comparable to those of blood. However, GSK2982772 has low brain penetration in rat (4%) despite possessing good cell permeability (21×10-6 cm/s)[1]. | | 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. |
| | GSK2982772 Preparation Products And Raw materials |
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