PF-9184 是一种有效且高度选择性的人微粒体前列腺素 E 合酶 1 (mPGES-1) 的抑制剂，IC50 值为 16.5 nM。PF-9184 体外抑制 IL-1β 诱导的 PGE2 合成。

PF-9184 is a potent and selective inhibitor of human microsomal prostaglandin E synthase-1 (mPGES-1), IC50 =16.5 nM. PF-9184 inhibits IL-1β-induced PGE2 synthesis 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. 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. 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. PF-9184 is a poor inhibitor of recombinant rat mPGES-1 (IC50=1080±398 nM)[1].

PF-9184 (oral administration or even local delivery) has no effect on PGE2 synthesis in recombinant rats[1].

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C21H14Cl2N2O4S

461.32

DMSO:10 mg/mL (21.7 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years