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PF-9184

Catalog No. T21738   CAS 1221971-47-6
Synonyms: PF9184, PF 9184

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.

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PF-9184, CAS 1221971-47-6
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Purity: 98%
Biological Description
Chemical Properties
Storage & Solubility Information
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 (oral administration or even local delivery) has no effect on PGE2 synthesis in recombinant rats[1].
Synonyms PF9184, PF 9184
Molecular Weight 461.32
Formula C21H14Cl2N2O4S
CAS No. 1221971-47-6

Storage

Powder: -20°C for 3 years In solvent: -80°C for 2 years

Solubility Information

DMSO: 10 mg/mL (21.7 mM), Need ultrasonic

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Citations

References and Literature
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.

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