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A7744458

GSK2982772 , 10mMinDMSO , 1622848-92-3

CAS NO.:1622848-92-3

Empirical Formula: C20H19N5O3

Molecular Weight: 377.4

MDL number: MFCD30489467

Pack Size Price Stock Quantity
1ml RMB573.60 In Stock
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Update time: 2022-07-08

PRODUCT 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.
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

Description and Uses

(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.

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].

Safety

Symbol(GHS) 
GHS07
Signal word  Warning
Hazard statements  H302-H315-H319-H335
Precautionary statements  P261-P305+P351+P338

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