| Description | 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. |
| 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]. |
| In vivo | PF-9184（口服或局部给药）对重组大鼠[1]的PGE2合成没有影响。 |
| molecular weight | 461.32 |
| Molecular formula | C21H14Cl2N2O4S |
| CAS | 1221971-47-6 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 60 mg/mL (130.06 mM), Sonication is recommended. |
| References | 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. |