Ebopiprant (OBE022) is an oral and selective prostaglandin F_2α(PGF_2α) receptor antagonist, withK_isof 1 nM, 26 nM for human and ratFPreceptors, respectively.

Ebopiprant (OBE022) and OBE002 are assayed for FP binding affinity by competitive binding analysis with 3H-PGF2α using HEK293 cells stably transfected with the FP receptor. Binding affinities (K_i) of OBE022 for the human and rat FP receptor are 1 nM and 26 nM respectively. For OBE002, K_is are 6 nM for the human and 313 nM for the rat FP receptor. The binding of both OBE022 and OBE002 is reversible and competitive since increasing concentrations of either compound causes successive decreases in the slope of the binding curves, consistent with an increase in equilibrium dissociation constant (K_D) without a reduction in receptor density^[1].

Time-course of the cumulative percentage of delivers mice after RU486-induced preterm parturition at GD17, in OBE022, nifedipine or vehicle treatment groups. Oral treatment with OBE022 delays the preterm birth caused by RU486 administration as reflected by a shift to the right of the percentage of delivery curve. The effect of oral treatment with nifedipine is comparable. Both OBE022 and nifedipine show a trend to increase the time of first pup delivery. As an important consequence of the prolongation of gestation, dams deliver viable pups. Combination of OBE022 and nifedipine cause a synergistic effect on the delay of RU486-induced preterm birth as reflected by a more pronounced shift to the right of the percentage of delivery curve, in comparison to OBE022 or nifedipine alone. Also, a larger increase of the time of first pup delivery is observed^[1].

599.74

Solid

C₃₀H₃₄FN₃O₅S₂

2005486-31-5

Room temperature in continental US; may vary elsewhere.

DMSO : 250 mg/mL(416.85 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℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。

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 (3.47 mM); Clear solution

  此方案可获得 ≥ 2.08 mg/mL (3.47 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% (20%SBE-β-CDin saline)

  Solubility: 2.08 mg/mL (3.47 mM); Suspended solution; Need ultrasonic

  此方案可获得 2.08 mg/mL (3.47 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。

  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 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

  将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
• 3.

  请依序添加每种溶剂： 10% DMSO    90%corn oil

  Solubility: ≥ 2.08 mg/mL (3.47 mM); Clear solution

  此方案可获得 ≥ 2.08 mg/mL (3.47 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。