GSK2982772
- Product Name
- GSK2982772
- CAS No.
- 1622848-92-3
- Chemical Name
- GSK2982772
- Synonyms
- 5184;CS-2502;GSK'772;GSK2982772;GSK2982772 98%min;GSK 2982772;GSK-2982772;RIP1 inhibitor GS2982772;GSK2982772, 10 mM in DMSO;(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;5-benzyl-N-[(3S)-5-methyl-4-oxo-2,3,4,5-tetrahydro-1,5-benzoxazepin-3-yl]-1H-1,2,4-triazole-3-carboxamide
- CBNumber
- CB53060417
- Molecular Formula
- C20H19N5O3
- Formula Weight
- 377.4
- MOL File
- 1622848-92-3.mol
GSK2982772 Property
- 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.
- InChIKey
- LYPAFUINURXJSG-AWEZNQCLSA-N
- SMILES
- N1C(C(N[C@@H]2C(=O)N(C)C3=CC=CC=C3OC2)=O)=NC(CC2=CC=CC=C2)=N1
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- 29230
- Product name
- GSK2982772
- Packaging
- 1mg
- Price
- $62
- Updated
- 2024/03/01
- Product number
- 29230
- Product name
- GSK2982772
- Packaging
- 10mg
- Price
- $357
- Updated
- 2024/03/01
- Product number
- 29230
- Product name
- GSK2982772
- Packaging
- 5mg
- Price
- $239
- Updated
- 2024/03/01
- Product number
- BG166667
- Product name
- GSK 2982772
- Packaging
- 10mg
- Price
- $250
- Updated
- 2021/12/16
- Product number
- Axon2713
- Product name
- GSK2982772
- Purity
- 99%
- Packaging
- 2x5mg
- Price
- $308
- Updated
- 2021/12/16
GSK2982772 Chemical Properties,Usage,Production
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
Raw materials
Preparation Products
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View Lastest Price from GSK2982772 manufacturers
- Product
- GSK2982772 1622848-92-3
- Price
- US $1.00/KG
- Min. Order
- 1KG
- Purity
- 98%
- Supply Ability
- 1lg; 2kg; 5kg; 10kg; 100kg
- Release date
- 2019-08-31