ONO AE3 208
Chemical Name: 4-Cyano-2-[[2-(4-fluoro-1-naphthalenyl)-1-oxopropyl]amino]benzenebutanoic acid
Biological ActivityHigh affinity and selective EP4 receptor antagonist (Ki values are 1.3, 30, 790 and 2400 nM for EP4, EP3, FP and TP receptors respectively). Displays no affinity for EP1, EP2, DP or IP receptors (Ki >10 μM). Inhibits PGE2-induced IL-8 production in colonic epithelial caco-2 cells and attenuates PGE2 inhibition of natural killer T cell activation. Suppresses recovery from experimentally-induced colitis and stimulates CD4+ T cell proliferation in C57BL/6 mice. Also reduces metastasis of mammary tumor cells in a murine model of breast cancer. Orally active.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
Exosome-like nanoparticles from intestinal mucosal cells carry prostaglandin E2 and suppress activation of liver NKT cells.
Deng et al.
Prostaglandin E receptor EP4 antagonism inhibits breast cancer metastasis.
Ma et al.
Cancer Res., 2006;66:2923
Prostaglandin E2 couples through EP4 prostanoid receptors to induce IL-8 production in human colonic epithelial cell lines.
Dey et al.
The prostaglandin receptor EP4 suppresses colitis, mucosal damage and CD4 cell activation in the gut.
Kabashima et al.
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in vivo survival assay