1. GPCR/G Protein
  2. Prostaglandin Receptor
  3. Ebopiprant

Ebopiprant  (Synonyms: OBE022)

目录号: HY-112284 纯度: 98.65%
COA 产品使用指南

Ebopiprant (OBE022) 是一个口服的、前列腺素 F (PGF) 受体的选择性拮抗剂,其对人和大鼠 FP 受体的 Ki 值分别为 1 nM 和 26 nM。

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Ebopiprant Chemical Structure

Ebopiprant Chemical Structure

CAS No. : 2005486-31-5

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥5280
In-stock
1 mg ¥2181
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5 mg ¥4800
In-stock
10 mg ¥8000
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50 mg   询价  
100 mg   询价  

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Customer Review

查看 Prostaglandin Receptor 亚型特异性产品:

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

Ebopiprant (OBE022) is an oral and selective prostaglandin F (PGF) receptor antagonist, with Kis of 1 nM, 26 nM for human and rat FP receptors, respectively.

IC50 & Target[1]

Human FP Receptor

1 nM (Ki)

Rat FP Receptor

26 nM (Ki)

体外研究
(In Vitro)

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 (Ki) of OBE022 for the human and rat FP receptor are 1 nM and 26 nM respectively. For OBE002, Kis 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 (KD) without a reduction in receptor density[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
分子量

599.74

Formula

C30H34FN3O5S2

CAS 号
性状

固体

颜色

White to light yellow

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
细胞实验: 

DMSO 中的溶解度 : 250 mg/mL (416.85 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.6674 mL 8.3369 mL 16.6739 mL
5 mM 0.3335 mL 1.6674 mL 3.3348 mL
查看完整储备液配制表

* 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。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物实验:

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

  • 方案 一

    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); 澄清溶液

    此方案可获得 ≥ 2.08 mg/mL(饱和度未知)的澄清溶液。

    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;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

    生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
  • 方案 二

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 2.08 mg/mL (3.47 mM); 悬浊液; 超声助溶

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

    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 20% 的 SBE-β-CD 生理盐水水溶液 中,混合均匀。

    20% SBE-β-CD in Saline 的配制(4°C,储存一周):2 g SBE-β-CD(磺丁基醚 β-环糊精)粉末定容于 10 mL 的生理盐水中,完全溶解至澄清透明。
动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
请输入您的动物体内配方组成:
%
DMSO +
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。
您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
连续给药周期超过半月以上,请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
纯度 & 产品资料
参考文献
Animal Administration
[1]

Mice[1]
Primigravid CD1 mice, on day 17 of pregnancy (about 85% gestation) at the beginning of the experiments, are used. Approximately 3 hours before induction of preterm labor (Day 1 (D1) at 10h00), the pregnant mice at gestational day 17, are placed in individual cages with food and water ad libitum. Pregnant mice receive on D1 (at day time: 13h00) a single subcutaneous (s.c.) injection of RU486 at a dose of 2.5 mg/kg in a final volume of 10 mL/kg of sesame oil. OBE022 (10, 30 and 100 mg/kg) or nifedipine (5 mg/kg) are administered orally (p.o.) at a volume of 5 mL/kg once on D1 (18h00), twice on D2 (8h00 and 18h00) and once on D3 (8h00) for a total of 4 administrations. For combination treatment, mice receive OBE022 plus nifedipine using the same experimental design as single treatment[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献

Ebopiprant 相关分类

完整储备液配制表

* 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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.6674 mL 8.3369 mL 16.6739 mL 41.6847 mL
5 mM 0.3335 mL 1.6674 mL 3.3348 mL 8.3369 mL
10 mM 0.1667 mL 0.8337 mL 1.6674 mL 4.1685 mL
15 mM 0.1112 mL 0.5558 mL 1.1116 mL 2.7790 mL
20 mM 0.0834 mL 0.4168 mL 0.8337 mL 2.0842 mL
25 mM 0.0667 mL 0.3335 mL 0.6670 mL 1.6674 mL
30 mM 0.0556 mL 0.2779 mL 0.5558 mL 1.3895 mL
40 mM 0.0417 mL 0.2084 mL 0.4168 mL 1.0421 mL
50 mM 0.0333 mL 0.1667 mL 0.3335 mL 0.8337 mL
60 mM 0.0278 mL 0.1389 mL 0.2779 mL 0.6947 mL
80 mM 0.0208 mL 0.1042 mL 0.2084 mL 0.5211 mL
100 mM 0.0167 mL 0.0834 mL 0.1667 mL 0.4168 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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HY-112284
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