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.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
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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MG-63 cells were treated with LPA (10 µM) alone or in combination with C3 (20 µM), PTX (Pertussis Toxin, 400 ng/ml) or H2L 5765834 (20 µM) for 3 h to follow COX-2 expression using Western blot. C3 inhibited COX-2 expression induced by LPA.