EP2 receptor antagonist-3
Based on 1 Customer Validation
EP2 receptor antagonist-3 is a selective EP2 receptor antagonist (IC50: 8 nM in hEP2 SPA assay, 50 nM in hEP2 cAMP assay). EP2 receptor antagonist-3 increases the macrophage-mediated clearance of Amyloid-β plaques. EP2 receptor antagonist-3 can be used for the study of alzheimer’s diseases.
For research use only. We do not sell to patients.
- Purity: 99.08%
- CAS No.: 1799626-16-6
- Formula: C23H19ClFN3O2
- Molecular Weight:423.87
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Membrane Protein-targeted Compound Library
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Membrane Receptor-targeted Compound Library
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Highly Selective Inhibitors Library
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Macrophage Related Compound Library
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Bioactive Compound Library Max
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MCE Bioactive Compound Library
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High-Throughput Bioactive Compound Library
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Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| ECV-304 | IC50 |
>30 μM
Compound: 52
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Displacement of [3H]-PGE2 from human EP1 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
Displacement of [3H]-PGE2 from human EP1 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
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[PMID: 26061158] |
| ECV-304 | IC50 |
>30 μM
Compound: 52
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Displacement of [3H]-PGE2 from human EP3 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
Displacement of [3H]-PGE2 from human EP3 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
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[PMID: 26061158] |
| ECV-304 | IC50 |
0.004 μM
Compound: 52
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Antagonist activity at mouse EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
Antagonist activity at mouse EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
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[PMID: 26061158] |
| ECV-304 | IC50 |
0.008 μM
Compound: 52
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Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
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[PMID: 26061158] |
| ECV-304 | IC50 |
0.01 μM
Compound: 52
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Displacement of [3H]-PGE2 from mouse EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
Displacement of [3H]-PGE2 from mouse EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
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[PMID: 26061158] |
| ECV-304 | IC50 |
0.01 μM
Compound: 52
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Displacement of [3H]-PGE2 from rat EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
Displacement of [3H]-PGE2 from rat EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
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[PMID: 26061158] |
| ECV-304 | IC50 |
0.03 μM
Compound: 52
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Antagonist activity at rat EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
Antagonist activity at rat EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
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[PMID: 26061158] |
| ECV-304 | IC50 |
0.05 μM
Compound: 52
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Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
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[PMID: 26061158] |
| ECV-304 | IC50 |
30 μM
Compound: 52
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Displacement of [3H]-PGE2 from human EP4 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
Displacement of [3H]-PGE2 from human EP4 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
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[PMID: 26061158] |
EP2 receptor antagonist-3 (Benzoxazepine 52) demonstrates potency across the human, rat, and mouse EP2 receptors in SPA assay with IC50s of 0.008 μM, 0.01 μM, 0.01 μM, respectively and in cAMP assay with IC50s of 0.05 μM, 0.03 μM, 0.004 μM, respectively[1].
EP2 receptor antagonist-3 (0.001-3.0 μM, 24 h) demonstrates a consistent dose-dependent increase in the IC21-mediated phagocytosis of Aβ plaques present on brain slices from 18 month old Tg2576 mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1799626-16-6
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Appearance Solid
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Molecular Weight 423.87
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Formula C23H19ClFN3O2
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Color White to off-white
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SMILES
O=C1C=C(CN2CC3=CC(N4C=CC5=C4C=CC(F)=C5)=CC(Cl)=C3OCC2)C=CN1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (235.92 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.90 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (272 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.3592 mL | 11.7961 mL | 23.5921 mL | 58.9803 mL |
| 5 mM | 0.4718 mL | 2.3592 mL | 4.7184 mL | 11.7961 mL | |
| 10 mM | 0.2359 mL | 1.1796 mL | 2.3592 mL | 5.8980 mL | |
| 15 mM | 0.1573 mL | 0.7864 mL | 1.5728 mL | 3.9320 mL | |
| 20 mM | 0.1180 mL | 0.5898 mL | 1.1796 mL | 2.9490 mL | |
| 25 mM | 0.0944 mL | 0.4718 mL | 0.9437 mL | 2.3592 mL | |
| 30 mM | 0.0786 mL | 0.3932 mL | 0.7864 mL | 1.9660 mL | |
| 40 mM | 0.0590 mL | 0.2949 mL | 0.5898 mL | 1.4745 mL | |
| 50 mM | 0.0472 mL | 0.2359 mL | 0.4718 mL | 1.1796 mL | |
| 60 mM | 0.0393 mL | 0.1966 mL | 0.3932 mL | 0.9830 mL | |
| 80 mM | 0.0295 mL | 0.1475 mL | 0.2949 mL | 0.7373 mL | |
| 100 mM | 0.0236 mL | 0.1180 mL | 0.2359 mL | 0.5898 mL |
EP2 receptor antagonist-3 Related Classifications
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