| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg | |||
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| Targets |
Ebopiprant targets the prostaglandin F2alpha (PGF2alpha) receptor (FP receptor), a G protein-coupled receptor that mediates the actions of PGF2alpha. PGF2alpha is a lipid mediator involved in various physiological processes, including uterine contraction during labor. Ebopiprant binds to the human FP receptor with a Ki of 1 nM and to the rat FP receptor with a Ki of 26 nM. By antagonizing the FP receptor, Ebopiprant blocks PGF2alpha-mediated signaling, thereby inhibiting uterine contractions.
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| ln Vitro |
Using HEK293 cells that were transfected with the FP receptor and subjected to a competitive binding experiment with 3H-PGF2α, the FP binding affinity of Ebopiprant (OBE022) and OBE002 was ascertained. OBE022 has binding affinities (Ki) of 1 nM for human and 26 nM for rat FP receptors, respectively. The Ki values for OBE002 are 6 nM for the human FP receptor and 313 nM for the rat FP receptor. OBE022 and OBE002 bind reversibly and competitively because, when the concentration of either compound is increased, the slope of the binding curve continuously decreases. This is consistent with an increase in the equilibrium dissociation constant (KD) without a corresponding decrease in receptor density [1].
In vitro, Ebopiprant functions as a potent and selective prostaglandin F2alpha (PGF2alpha) receptor antagonist. The compound binds to the human FP receptor with a Ki of 1 nM and to the rat FP receptor with a Ki of 26 nM. Ebopiprant interferes with PGF2alpha binding to the FP receptor, blocking downstream signaling. These in vitro properties establish Ebopiprant as a valuable tool for studying PGF2alpha receptor biology and for therapeutic applications in preterm labor. |
| ln Vivo |
Time course of cumulative percent delivery in mice treated with OBE022, nifedipine, or vehicle following RU486-induced GD17 preterm birth. An oral OBE022 medication postponed the RU486-induced preterm labor, as evidenced by a shift to the right in the percent labor curve. Oral therapy is equally efficacious as nifedipine. The duration until the first pup delivery increased in both OBE022 and nifedipine. One significant outcome of the longer gestation period is that the mother rat can give birth to healthy pups. When compared to OBE022 or nifedipine alone, there was a more noticeable shift to the right in the percentage labor curve, indicating that the combination of the two medications worked synergistically to postpone RU486-induced preterm labor. Furthermore, a significant increase in the first pup's birth time was noted [1].
In vivo, Ebopiprant has been studied as an effective and safe modality for the treatment of preterm labor. As an orally bioavailable PGF2alpha receptor antagonist, the compound inhibits uterine contractions by blocking PGF2alpha-mediated signaling. Detailed in vivo efficacy data are available in the scientific literature. Ebopiprant is for research purposes only and is not approved for clinical use. |
| Enzyme Assay |
Receptor binding assays for Ebopiprant are performed using membranes from cells expressing human or rat FP receptors. Radioligand binding experiments are conducted using [3H]PGF2alpha or other appropriate radioligands. Membranes are incubated with varying concentrations of Ebopiprant and a fixed concentration of radioligand in binding buffer at room temperature or 4degC for a defined incubation period. Nonspecific binding is determined in the presence of excess unlabeled PGF2alpha. Bound and free radioligands are separated by filtration, and radioactivity is measured by scintillation counting to calculate Ki values.
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| Cell Assay |
Cellular assays for Ebopiprant are performed using cell lines expressing FP receptors, such as human myometrial cells or heterologous expression systems. Cells are cultured in appropriate media and treated with Ebopiprant at varying concentrations. Receptor activation is assessed by measuring second messenger responses such as intracellular calcium mobilization following stimulation with PGF2alpha. The compound's antagonist activity is assessed by its ability to inhibit PGF2alpha-induced responses. Cell viability is assessed using standard assays such as MTT or CellTiter-Glo.
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| Animal Protocol |
In vivo studies with Ebopiprant are conducted in animal models of preterm labor. Ebopiprant is administered via oral routes at defined doses and schedules. Uterine contractions are measured using invasive or non-invasive techniques. The compound's ability to inhibit preterm labor and prolong pregnancy is assessed. Pharmacokinetic parameters are determined from plasma samples collected at various time points. Ebopiprant has been studied for its efficacy and safety in preclinical models.
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| ADME/Pharmacokinetics |
Ebopiprant has a molecular weight of 466.6 and a molecular formula of C27H30N2O5. The compound is orally bioavailable. Ebopiprant binds to the human FP receptor with a Ki of 1 nM and to the rat FP receptor with a Ki of 26 nM. Detailed pharmacokinetic parameters, including oral bioavailability and half-life, have been characterized in preclinical studies. The compound is soluble in DMSO. It should be stored at -20degC.
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| Toxicity/Toxicokinetics |
Comprehensive toxicology data for Ebopiprant are documented in preclinical studies. The compound is intended for research use only and is not approved for human therapeutic applications. Standard laboratory safety practices should be followed when handling this compound, including the use of appropriate personal protective equipment and adherence to institutional biosafety and chemical hygiene guidelines. The compound has a purity of ≥98%.
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| References | |
| Additional Infomation |
Ebopiprant is being investigated in the clinical trial NCT03369262 (OBE022 Poc Study in Threatened Preterm Labor).
Ebopiprant (OBE022) is a first-in-class, potent, orally bioavailable and selective prostaglandin F2alpha (PGF2alpha) receptor antagonist. It binds to the human FP receptor with a Ki of 1 nM and to the rat FP receptor with a Ki of 26 nM. Ebopiprant has been studied as an effective and safe modality for the treatment of preterm labor. The compound is for research purposes only. |
| Molecular Formula |
C30H34FN3O5S2
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|---|---|
| Molecular Weight |
599.736468791962
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| Exact Mass |
599.192
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| CAS # |
2005486-31-5
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| Related CAS # |
2005486-31-5;2005486-32-6 (HCl);2005486-34-8 (fumarate);2005486-33-7 (sulfate); 2005486-42-8; 2005486-37-1 (citrate); 2005486-38-2 (esylate);
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| PubChem CID |
122522051
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| Appearance |
White to light yellow solid powder
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| LogP |
4.9
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
12
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| Heavy Atom Count |
41
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| Complexity |
956
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| Defined Atom Stereocenter Count |
3
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| SMILES |
S(C1C=CC(C2C=CC=CC=2)=CC=1)(N1CCS[C@H]1C(N[C@H](C1C=CC(=CC=1)F)CCOC([C@H](C(C)C)N)=O)=O)(=O)=O
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| InChi Key |
UUIBKACUTXYSAK-YCVJPRETSA-N
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| InChi Code |
InChI=1S/C30H34FN3O5S2/c1-20(2)27(32)30(36)39-18-16-26(23-8-12-24(31)13-9-23)33-28(35)29-34(17-19-40-29)41(37,38)25-14-10-22(11-15-25)21-6-4-3-5-7-21/h3-15,20,26-27,29H,16-19,32H2,1-2H3,(H,33,35)/t26-,27-,29-/m0/s1
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| Chemical Name |
[(3S)-3-(4-fluorophenyl)-3-[[(2S)-3-(4-phenylphenyl)sulfonyl-1,3-thiazolidine-2-carbonyl]amino]propyl] (2S)-2-amino-3-methylbutanoate
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~250 mg/mL (~416.85 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (3.47 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.08 mg/mL (3.47 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (3.47 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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