OBE022
(Synonyms: OBE022) 目录号 : GC32413
OBE022 (OBE022) 是一种口服选择性前列腺素 F2α； (PGF2α) 受体拮抗剂，对人和大鼠 FP 受体的 Kis 分别为 1 nM 和 26 nM。
Cas No.:2005486-31-5
Sample solution is provided at 25 µL, 10mM.
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OBE022 is an oral and selective prostaglandin F2α (PGF2α) receptor antagonist, with Kis of 1 nM, 26 nM for human and rat FP receptors, respectively.
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].
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].
[1]. Oliver Pohl, et al. OBE022, an oral and selective prostaglandin F2α receptor antagonist as an effective and safe modality for the treatment of preterm labor. J Pharmacol Exp Ther. 2018 Aug;366(2):349-364.
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Animal experiment: |
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]. |
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References: [1]. Oliver Pohl, et al. OBE022, an oral and selective prostaglandin F2α receptor antagonist as an effective and safe modality for the treatment of preterm labor. J Pharmacol Exp Ther. 2018 Aug;366(2):349-364. |
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| Cas No. | 2005486-31-5 | SDF | |
| 别名 | OBE022 | ||
| Canonical SMILES | O=C(N[C@H](C1=CC=C(F)C=C1)CCOC([C@H](C(C)C)N)=O)[C@H](SCC2)N2S(C(C=C3)=CC=C3C4=CC=CC=C4)(=O)=O | ||
| 分子式 | C30H34FN3O5S2 | 分子量 | 599.74 |
| 溶解度 | DMSO : 250 mg/mL | 储存条件 | Store at -20°C |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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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 |
| 10 mM | 0.1667 mL | 0.8337 mL | 1.6674 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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Quality Control & SDS
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- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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