| 产品描述: | ONO-AE3-208 is a selective and orally active EP4 receptor antagonist with a Ki of 1.3 nM. ONO-AE3-208 shows less potently affects EP3, FP, and TP receptors (Ki of 30 nM, 790 nM, and 2400 nM, respectively). ONO-AE3-208 suppresses cell invasion, migration, and metastasis of prostate cancer |
| 靶点: |
FP:790 nM (Ki);TP Receptor:2400 nM (Ki);EP4:1.3 nM (Ki);EP3:30 nM (Ki);ProstaglandinReceptor |
| 体内研究: |
ONO-AE3-208 surpresses the in vivo bone metastasis of PC3 cells in mice. The photon tumor burdens are significantly increased in a time-dependent manner in the control group in comparison with those in the ONO-AE3-208-treated group. The rate of metastasis formation is significantly higher in the former than in the latter. The median time of metastasis formation is 29 d in the ONO-AE3-208-treated animals as compared with 21 d in the controls |
| 参考文献: |
1. Kenji Kabashima, et al. The prostaglandin receptor EP4 suppresses colitis, mucosal damage and CD4 cell activation in the gut. J Clin Invest. 2002 Apr;109(7):883-93. 2. Ren Y, et al. Prostaglandin E2 mediates connecting tubule glomerular feedback. Hypertension. 2013 Dec;62(6):1123-8. 3. Xu S, et al. An EP4 Antagonist ONO-AE3-208 Suppresses Cell Invasion, Migration, and Metastasis of Prostate Cancer. Cell Biochem Biophys. 2014 Apr 18. 4. Xu S, et al. Inhibitory effect of ONO-AE3-208 on the formation of bone metastasis of prostate cancer in mice. Zhonghua Nan Ke Xue. 2014 Aug;20(8):684-9. 5. Thieme K, et al. EP4 inhibition attenuates the development of diabetic and non-diabetic experimental kidney disease. Sci Rep. 2017 Jun 13;7(1):3442. |
| 溶解性: |
Soluble in DMSO |
| 保存条件: |
-20℃ |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
2.473 ml |
12.363 ml |
24.726 ml |
| 5 mM |
0.495 ml |
2.473 ml |
4.945 ml |
| 10 mM |
0.247 ml |
1.236 ml |
2.473 ml |
| 50 mM |
0.049 ml |
0.247 ml |
0.495 ml |
|
| 注意: |
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