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PH797804

PH797804 structure

PH797804 

structure
  • CAS No:

    586379-66-0

  • Formula:

    C22H19BrF2N2O3

  • Chemical Name:

    PH797804

  • Synonyms:

    Benzamide,3-[3-bromo-4-[(2,4-difluorophenyl)methoxy]-6-methyl-2-oxo-1(2H)-pyridinyl]-N,4-dimethyl-;3-[3-Bromo-4-[(2,4-difluorophenyl)methoxy]-6-methyl-2-oxo-1(2H)-pyridinyl]-N,4-dimethylbenzamide;3-Bromo-4-[(2,4-difluorobenzyl)oxy]-1-[5-[(methylamino)carbonyl]-2-methylphenyl]-6-methylpyridin-2(1H)-one;PH 797804;1073667-47-6

  • Categories:

    Biochemical Engineering  >  Inhibitors

Description

PH-797804 is a novel pyridinone inhibitor of p38α with IC50 of 26 nM; 4-fold more selective versus p38β and does not inhibit JNK2.IC50 value: 26 nM [1]Target: p38αMAPKin vitro: PH-797804 blocks LPS-induced TNF-α production and p38 kinase activity in the human monocytic U937 cell line, with comparable IC50 of 5.9 nM and 1.1 nM. PH-797804 has no inhibitory effect on either the JNK pathway (c-Jun phosphorylation) or ERK pathway (ERK phosphorylation) in U937 cells at concentrations up to 1 μ


PH 797804 is a member of the class of benzamides obtained by formal condensation of the carboxy group of 3-{3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1-yl}-4-methylbenzoic acid with the amino group of methylamine. It has a role as an EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor and an anti-inflammatory agent. It is a member of benzamides, an organofluorine compound, a pyridone, an organobromine compound and an aromatic ether.|PH-797804 has been investigated for the treatment of Osteoarthritis.

PH797804 Basic Attributes

477.2986664

477.30

SI09I1V827|GEL7GRJ3R6

DTXSID70207342

2933399090

Characteristics

58.6

3.24

1.5±0.1 g/cm3

593.2±50.0 °C at 760 mmHg

312.6±30.1 °C

1.629

Drug Information

PH 797804

PH797804 Use and Manufacturing

PH-797804 is a novel N-phenylpyridinone inhibitor of p38 mitogen-activated protein (MAP) kinase derived from a racemic mixture as the more potent atropisomer and is also known to exerts anti-inflammatory properties.

Computed Properties

Molecular Weight:477.3
XLogP3:4.2
Hydrogen Bond Donor Count:1
Hydrogen Bond Acceptor Count:5
Rotatable Bond Count:5
Exact Mass:476.05471
Monoisotopic Mass:476.05471
Topological Polar Surface Area:58.6
Heavy Atom Count:30
Complexity:742
Covalently-Bonded Unit Count:1
Compound Is Canonicalized:Yes

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