ONO AE3 208
High 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.
|Storage||Store at -20°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
|1.1eq. NaOH||4.04||10 with gentle warming|
Preparing Stock Solutions
The following data is based on the product molecular weight 404.43. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||2.47 mL||12.36 mL||24.73 mL|
|5 mM||0.49 mL||2.47 mL||4.95 mL|
|10 mM||0.25 mL||1.24 mL||2.47 mL|
|50 mM||0.05 mL||0.25 mL||0.49 mL|
References are publications that support the biological activity of the product.
Ma et al (2006) Prostaglandin E receptor EP4 antagonism inhibits breast cancer metastasis. Cancer Res. 66 2923 PMID: 16540639
Dey et al (2009) Prostaglandin E2 couples through EP4 prostanoid receptors to induce IL-8 production in human colonic epithelial cell lines. Br.J.Pharmacol 3 475 PMID: 19175605
Kabashima et al (2002) The prostaglandin receptor EP4 suppresses colitis, mucosal damage and CD4 cell activation in the gut. J.Clin.Invest. 109 883 PMID: 11927615
Deng et al (2013) Exosome-like nanoparticles from intestinal mucosal cells carry prostaglandin E2 and suppress activation of liver NKT cells. J.Immunol. 190 3579 PMID: 23467936
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in vivo survival assay
Literature in this Area
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Peripheral sensitization is the reduction in the threshold of excitability of sensory neurons that results in an augmented response to a given external stimulus. This poster outlines the excitatory and inhibitory signaling pathways involved in modulation of peripheral sensitization. The role of ion channels, GPCRs, neurotrophins, and cytokines in sensory neurons are also described.