ONO-AE3-208 is a selective and orally active EP4 receptor antagonist with a K_i of 1.3 nM. ONO-AE3-208 shows less potently affects EP3, FP, and TP receptors (K_i of 30 nM, 790 nM, and 2400 nM, respectively). ONO-AE3-208 suppresses cell invasion, migration, and metastasis of prostate cancer^[1][2].

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

404.43

C₂₄H₂₁FN₂O₃

402473-54-5

Room temperature in continental US; may vary elsewhere.

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

In Vitro: 

DMSO : 33.33 mg/mL (82.41 mM; Need ultrasonic)

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

• 1.

  请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

  Solubility: ≥ 2.08 mg/mL (5.14 mM); Clear solution

  此方案可获得 ≥ 2.08 mg/mL (5.14 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

  将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

• 2.

  请依序添加每种溶剂： 10% DMSO    90% corn oil

  Solubility: ≥ 2.08 mg/mL (5.14 mM); Clear solution

  此方案可获得 ≥ 2.08 mg/mL (5.14 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

  以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

• [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.