Chemical Name: N-Cyclopentyl-1-[5,6-dimethyl-1-(1-methylethyl)-1H-benzimidazol-2-yl]-4-piperidinecarboxamide
Biological ActivitySelective microsomal prostaglandin E synthase 1 (mPGES-1) inhibitor (IC50 values are 90 and 900 nM for rat and human mPGES-1, respectively). Displays selectivity for mPGES-1 over COX-1, COX-2, PGIS, hPGDS and iPGDS (% inhibition values are 15, 18, 0, 0 and 60 % inhibition at 50 μM, respectively). Reduces PGE2 production in vitro and in a localized inflammation animal model. Elevates CD80 expression by tumor associated phagocytes in vitro. Also decreases vascular contractility, in ex vivo human vessels.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Characterization of a human and murine mPGES-1 inhibitor and comparison to mPGES-1 genetic deletion in mouse models of inflammation.
Leclerc et al.
Prostaglandins Other Lipid Mediat., 2013;107:26
Inhibition of microsomal PGE synthase-1 reduces human vascular tone by increasing PGI2: a safer alternative to COX-2 inhibition.
Ozen et al.
MPGES-1-derived PGE2 suppresses CD80 expression on tumor-associated phagocytes to inhibit anti-tumor immune responses in breast cancer.
Olesch et al.
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