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Submit ReviewONO AE3 208 is a 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.
分子量 | 404.43 |
公式 | C24H21FN2O3 |
储存 | Store at -20°C |
纯度 | ≥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 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 40.44 | 100 |
以下数据基于产品分子量 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.
浓度/溶剂体积/质量 | 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 |
参考文献是支持产品生物活性的出版物。
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
If you know of a relevant reference for ONO AE3 208, please let us know.
关键词: ONO AE3 208, ONO AE3 208 supplier, ONOAE3208, selective, EP4, receptors, antagonists, prostanoids, PGE2, prostaglandins, high, affinity, orally, active, Prostanoid, Receptors, 3565, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 ONO AE3 208 的部分引用包括:
David M et al (2020) The transition of M-CSF-derived human macrophages to a growth-promoting phenotype. Blood Adv 4 5460-5472 PMID: 33166408
Na-Ryum et al (2023) An airway-to-brain sensory pathway mediates influenza-induced sickness. Nature 615 660-667 PMID: 36890237
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