Biochem/physiol Actions
PGE2 is involved in inflammation and is one of the most abundant prostanoid.
PF-03549184 (PF-9184) is a potent inhibitor of microsomal prostaglandin E synthase-1 (mPGES-1) with an IC50 value of 16.5 nM in recombinant human mPGES-1. mPEGS-1 is the terminal enzyme that synthesizes prostaglandin E2 (PGE2) from PGH2 to PGE2 downstream of cyclooxygenase-2 (COX-2). Its expression is induced in response to pro-inflammatory mediators, similar to COX-2. Unlike the effects of COX inhibition, PF-9184 does not inhibit the production of other PGH2-derived products such as 6-keto-PGFα or PGF2α. PF-9184 inhibits PGE2 production in cell based assays with IC50 ranges from 0.5 to 5 µM. IC50 concentrations for rhCOX1 and rHCOX2 are 118 µM and 236 µM, respectively.
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Sold for research purposes under agreement from Pfizer Inc.
Other Notes
This compound was developed by Pfizer for Lipid Signaling research. To learn more about Sigma′s partnership with Pfizer and view other authentic, high-quality Pfizer compounds, visit sigma.com/bsm-pfizer.
Packaging
5, 25 mg in glass bottle
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