ONO AE3 208

Biological Activity

High affinity and selective EP₄ receptor antagonist (K_i 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 (K_i >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.

Technical Data

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

1. Exosome-like nanoparticles from intestinal mucosal cells carry prostaglandin E2 and suppress activation of liver NKT cells.
   Deng et al.
   J.Immunol., 2013;190:3579
2. Prostaglandin E receptor EP₄ antagonism inhibits breast cancer metastasis.
   Ma et al.
   Cancer Res., 2006;66:2923
3. Prostaglandin E₂ couples through EP₄ prostanoid receptors to induce IL-8 production in human colonic epithelial cell lines.
   Dey et al.
   Br.J.Pharmacol, 2009;3:475
4. The prostaglandin receptor EP₄ suppresses colitis, mucosal damage and CD⁴ cell activation in the gut.
   Kabashima et al.
   J.Clin.Invest., 2002;109:883

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