Name | pf-9184 |
---|---|
Synonyms | N-(3',4'-dichlorobiphenyl-4-yl)-4-hydroxy-2H-1,2-benzothiazine-3-carboxamide 1,1-dioxide |
Description | PF-9184 is a potent and highly selective inhibitor of human microsomal prostaglandin E synthase-1 (mPGES-1), with an IC50 of 16.5 nM. PF-9184 inhibits IL-1β-induced PGE2 synthesis in vitro[1]. |
---|---|
Related Catalog | |
Target |
IC50: 16.5 nM (mPGES-1)[1] |
In Vitro | PF-9184 (0.015-100 μM; 24 hours) inhibits IL-1β-stimulated prostaglandin E2 (PGE2) synthesis in rheumatoid arthritis (RASF) in synovial fibroblasts derived from patients and has no apparent cytotoxic effects up to 100 μM[1]. PF-9184 (0.015-100 μM) potently blocks mPGES-1 ability to synthesize PGE2 from PGH2, and with no apparent inhibitory effects on COX-2 and prostacyclin synthase in cells[1]. PF-9184 (0.015-100 μM) inhibits PGE2 weakly but has no effect on TXB2 synthesis except at 100 μM in human whole blood and modified blood assays[1]. PF-9184 is a poor inhibitor of recombinant rat mPGES-1 (IC50=1080±398 nM)[1]. |
In Vivo | PF-9184 (oral administration or even local delivery) has no effect on PGE2 synthesis in recombinant rats[1]. |
References |
Molecular Formula | C21H14Cl2N2O4S |
---|---|
Molecular Weight | 461.31800 |
Exact Mass | 460.00500 |
PSA | 103.88000 |
LogP | 6.30020 |
Hazard Codes | Xi |
---|