PF-9184 

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].

IC50: 16.5 nM (mPGES-1)^[1]

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

461.32

C₂₁H₁₄Cl₂N₂O₄S

1221971-47-6

O=C(C1=C(O)C2=CC=CC=C2S(N1)(=O)=O)NC3=CC=C(C4=CC=C(Cl)C(Cl)=C4)C=C3

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Gabriel M, et, al. Distinction of microsomal prostaglandin E synthase-1 (mPGES-1) inhibition from cyclooxygenase-2 inhibition in cells using a novel, selective mPGES-1 inhibitor. Biochem Pharmacol. 2010 May 15; 79(10): 1445-54.  [Content Brief]