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Cat. No. Name Size Price Add Cart
KI3480PH-797804QuoteQuote

Chemical Characteristic

Product NamePH-797804
CAS No.586379-66-0
Molecular Weight 477.3
FormulaC22H19BrF2N2O3
Chemical Name3-[3-bromo-4-[(2,4-difluorophenyl)methoxy]-6-methyl-2-oxopyridin-1-yl]-N,4-dimethylbenzamide
SmilesC(=O)(c1cc(c(cc1)C)n1c(=O)c(c(cc1C)OCc1c(cc(cc1)F)F)Br)NC
Chemical Structure

Biological activities

PH-797804 is an inhibitor of the α isoform of human p38 mitogen-active protein kinase (MAPK). PH-797804 inhibits p38α kinase with an IC50 of 26 nM in human monocyte and synovial fibroblast cell systems.[1] PH-797804 blocks production of cytokines and proinflammatory mediators that are induced by inflammation in vitro. PH-797804 blocks LPS-stimulated p38 kinase activity with an IC50 of 1.1 nM in human monocytic U937 cells. PH-797804 inhibits RANKL- and M-CSF-induced osteoclast formation in a concentration-dependent manner, with an IC50 of 3 nM in primary rat bone marrow cells. PH-797804 inhibits acute inflammatory responses in vivo. In rats and cynomolgus monkeys in vivo, treatment of PH-797804 results in dose-dependent inhibition of LPS-induced TNF-α production.[1,2] PH-797804 treatment demonstrates robust anti-inflammatory activity in chronic disease models, significantly suppressing both joint inflammation and associated bone loss in rat streptococcal cell wall-induced arthritis and mouse collagen-induced arthritis models. Dose-response and concentration-response analysis data of PH-797804 shows the ED50 values of 0.07 and 0.095 mg/kg in LPS-induced TNF-α production models in rat and cynomolgus monkeys, respectively. PH-797804 modulates LPS-induced cytokines (TNF-α, IL-6) production and MK-2 activity in a dose- and concentration-dependent manner in a human endotoxin challenge model.[1]

Protocols

PH-797804 is dissolved in 0.5% methylcellulose and 0.025% Tween 20 in vivo.[1]

References

[1] Hope HR, Anderson GD, Burnette BL, Compton RP, et al. Anti-inflammatory properties of a novel N-phenyl pyridinone inhibitor of p38 mitogen-activated protein kinase: preclinical-to-clinical translation. J Pharmacol Exp Ther. 2009, 331(3):882-895.

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KareBayTM provides scientists and clinicians with a wide range of biotechnological products and science lab supplies for chemical research and analyzing life processes. KareBay's extensive capabilities include commercializing reagents and kits, manufacturing biotech products and providing contract research services to organizations worldwide. Our many global labs, offices, and business partners enable KareBay to extend its products and services to its customer base around the world.

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