Biological Activity
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.
Technical Data
| M. Wt | 404.43 |
| Formula | C24H21FN2O3 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 402473-54-5 |
| PubChem ID | 10111831 |
| InChI Key | MTDIMKNAJUQTIO-UHFFFAOYSA-N |
| Smiles | O=C(C(C)C2=C(C=CC=C3)C3=C(F)C=C2)NC1=CC(C#N)=CC=C1CCCC(O)=O |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| 1.1eq. NaOH | 4.04 | 10mM with gentle warming | |
| DMSO | 40.44 | 100 |
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 solvent 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 |
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Product Datasheets
References
References are publications that support the products' biological activity.
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
Keywords: ONO AE3 208, supplier, ONOAE3208, selective, EP4, receptors, antagonists, prostanoids, PGE2, prostaglandins, high, affinity, orally, active, prostanoids, Prostanoid, Receptors, Prostanoid, Receptors, Tocris Bioscience
