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Enzymes for Research, Diagnostic and Industrial Use

PH-797804

Cat No.
CEI-0157
Description
PH-797804 can inhibit p38 alpha with IC50 of 26 nM.
CAS No.
586379-66-0
Molecular Weight
477.3
Purity
>99%
Storage
2 years at -20 centigrade
Targets
p38 alpha
Molecular Formula
C22H19BrF2N2O3
Chemical Name
3-(4-(2,4-difluorobenzyloxy)-3-bromo-6-methyl-2-oxopyridin-1(2H)-yl)-N,4-dimethylbenzamide
Solubility
DSMO 96 mg/mL Water
In vitro
PH-797804 is a highly selective inhibitor of p38-alpha kinase with IC50 of 26 nM. PH-797804 can block the production of cytokines and proinflammatory mediators. PH-797804 was potent and efficacious in blocking cellular p38 kinase activity along with biological responses in human cells associated with inflammation in the arthritic joint. PH-797804 can inhibit LPS-stimulated TNF- alpha production and p38 kinase activity with IC50 of 5.9 and 1.1 nM.
In vivo
PH-797804 can suppress chronic inflammation in both an inflammatory arthritis model in rats induced by SCW extract and in the widely used mouse collageninduced arthritis model. Doses of 0.5 to 5 mg/kg PH-797804 produced almost complete protection of the joint against inflammation-related bone density loss, whereas doses of 0.05 and 0.15 mg/kg were partially efficacious.
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