High affinity and selective EP4
receptor antagonist (Ki
values are 1.3, 30, 790 and 2400 nM for EP4
, FP and TP receptors respectively). Displays no affinity for EP1
, DP or IP receptors (Ki
M). 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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All Tocris products are intended for laboratory research use only.
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.