| Bioactivity | 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[1][2]. | ||||||||||||
| Invitro | ONO-AE3-208 surpresses the in vitro cell invasion and migration in a dose-dependent manner without affecting cell proliferation[2]. ONO-AE3-208 abolisheS CTGF in the presence of the EET synthesis inhibitor MS-PPOH. Arachidonic acid (AA) causeS dose-dependent dilation of the attached Af-Art, and this effect is blocked by ONO-AE3-208[3]. | ||||||||||||
| In Vivo | ONO-AE3-208 surpresses the in vivo bone metastasis of PC3 cells in mice[2]. 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[4]. | ||||||||||||
| Name | ONO-AE3-208 | ||||||||||||
| CAS | 402473-54-5 | ||||||||||||
| Formula | C24H21FN2O3 | ||||||||||||
| Molar Mass | 404.43 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. |
ONO-AE3-208
CAS: 402473-54-5 F: C24H21FN2O3 W: 404.43
ONO-AE3-208 is a selective and orally active EP4 receptor antagonist with a Ki of 1.3 nM. ONO-AE3-208 shows less potentl
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