PH 797804
Chemical Name: (-)-3-[3-Bromo-4-[(2,4-difluorophenyl)methoxy]-6-methyl-2-oxo-1(2H)-pyridinyl]-N,4-dimethylbenzamide
Purity: ≥98%
Biological Activity
PH 797804 is a 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.PH 797804 is the (-)-atropisomer, which is 100-fold more potent than its (+)-atropisomer.
Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Additional Information
- PH 797804 is the (-)-atropisomer, which is 100-fold more potent than its (+)-atropisomer
Background References
-
Anti-inflammatory properties of a novel N-phenyl pyridinone inhibitor of p38 mitogen-activated protein kinase: preclinical-to-clinical translation.
Hope et al.
J.Pharmacol.Exp.Ther., 2009;331:882 -
Discovery of PH-797804, a highly selective and potent inhibitor of p38 MAP kinase.
Selness et al.
Bioorg.Med.Chem.Lett., 2011;21:4066
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