ONO AE3 208

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Cat.No. 3565 - ONO AE3 208 | C24H21FN2O3 | CAS No. 402473-54-5
Description: High affinity and selective EP4 antagonist
Chemical Name: 4-Cyano-2-[[2-(4-fluoro-1-naphthalenyl)-1-oxopropyl]amino]benzenebutanoic acid
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews (1)
Literature

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 10 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

Certificate of Analysis / Product Datasheet
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References

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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Keywords: ONO AE3 208, ONO AE3 208 supplier, ONOAE3208, selective, EP4, receptors, antagonists, prostanoids, PGE2, prostaglandins, high, affinity, orally, active, Prostanoid, Receptors, 3565, Tocris Bioscience

Citations for ONO AE3 208

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ONO AE3 208
By Anonymous on 05/31/2017

in vivo survival assay


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