PF-03549184，≥98% (HPLC)

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.

PGE2 is involved in inflammation and is one of the most abundant prostanoid.[1]

 

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.

 

Sold for research purposes under agreement from Pfizer Inc.

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