PH 797804

Cat. No. 5866

PH 797804 C22H19BrF2N2O3 [1358027-80-1]

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Chemical Name: (-)-3-[3-Bromo-4-[(2,4-difluorophenyl)methoxy]-6-methyl-2-oxo-1(2H)-pyridinyl]-N,4-dimethylbenzamide

Biological Activity

Potent and selective p38α/β inhibitor (IC50 values are 26 and 102 nM, respectively). Exhibits >100-fold selectivity for p38α/β over 71 other kinases, enzymes and GPCRs, including p38γ, p38δ, JNK and ERK2. Inhibits LPS-induced TNFα production in U937 monocytes in vitro. Suppresses acute and chronic inflammatory responses in rat models of arthritis. Orally active.

Licensing Information

Sold for research purposes under agreement from Pfizer Inc

Technical Data

M.Wt:
477.3
Formula:
C22H19BrF2N2O3
Solubility:
Soluble to 50 mM in DMSO
Purity:
>98 %
Storage:
Store at -20°C
CAS No:
1358027-80-1

Resources

Other Information

  • PH 797804 is the (-)-atropisomer, which is 100-fold more potent than its (+)-atropisomer

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Product Datasheet / Safety Datasheet

Selness et al (2011) Discovery of PH-797804, a highly selective and potent inhibitor of p38 MAP kinase. Bioorg.Med.Chem.Lett. 21 4066. PMID: 21641211.

Hope et al (2009) Anti-inflammatory properties of a novel N-phenyl pyridinone inhibitor of p38 mitogen-activated protein kinase: preclinical-to-clinical translation. J.Pharmacol.Exp.Ther. 331 882. PMID: 19720877.

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Keywords: PH 797804, supplier, PH797804, potent, selective, p38a, p38alpha, p38b, p38beta, p38α, p38β, inhibitors, inhibits, anti-inflammatory, Tocris Bioscience, p38 MAPK Inhibitor products

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