货号 | 3565/50 |
别名 | 4-Cyano-2-[[2-(4-fluoro-1-naphthale |
供应商 | Tocris |
生物活性 | 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>10μM). 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. |
运输条件 | Blue Ice |
存放说明 | -20℃ |
纯度 | >98 % |
计算分子量 | 404.43 |
分子式 | C24H21FN2O3< |
可溶性/溶解性 | Soluble to 100 mM in DMSO and to 10 mM in 1.1eq. NaOH with gentle warming |
参考文献 | Denget 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. Deyet 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. Maet al (2006) Prostaglandin E receptor EP4 antagonism inhibits breast cancer metastasis. Cancer Res. 66 2923. PMID: 16540639. Kabashimaet al (2002) The prostaglandin receptor EP4 suppresses colitis, mucosal damage and CD4 cell activation in the gut. J.Clin.Invest. 109 883. PMID: 11927615. |