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PH797804

Chemical Structure : PH797804

CAS No.: 586379-66-0

PH797804 (PH-797804)

Catalog No.: PC-21598Not For Human Use, Lab Use Only.

PH-797804 is a potent, highly selective and ATP-competitive p38α/p38β MAPK inhibitor with IC50 of 2.3 nM (p38α).

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

PH-797804 is a potent, highly selective and ATP-competitive p38α/p38β MAPK inhibitor with IC50 of 2.3 nM (p38α).
PH-797804 exhibits significant inhibition of TNFα release in hPBMC with IC50 of 3.4 nM.
PH-797804 is a readily reversible inhibitor of the alpha isoform of human p38 MAP kinase with Ki of 5.8 nM.
PH-797804 blocks inflammation-induced production of cytokines and proinflammatory mediators, such as prostaglandin E(2) in human monocyte and synovial fibroblast cell systems.
PH-797804 effectively inhibits acute inflammatory responses induced by systemically administered endotoxin in both rat and cynomolgus monkeys.
PH-797804 demonstrates robust anti-inflammatory activity in chronic disease models, significantly reducing both joint inflammation and associated bone loss in streptococcal cell wall-induced arthritis in rats and mouse collagen-induced arthritis.

Physicochemical Properties

M.Wt 477.31
Formula C22H19BrF2N2O3
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

3-[3-bromo-4-[(2,4-difluorophenyl)methoxy]-6-methyl-2-oxopyridin-1-yl]-N,4-dimethylbenzamide

References

1. Selness SR, et al. Bioorg Med Chem Lett. 2011 Jul 1;21(13):4066-71.

2. Hope HR, et al. J Pharmacol Exp Ther. 2009 Dec;331(3):882-95.

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