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EP2 receptor antagonist-3 is a selective antagonist of the EP2 receptor, with an IC50 of 8 nM determined in the hEP2 SPA assay and an IC50 of 50 nM in the hEP2 cAMP assay. It enhances macrophage-mediated clearance of Amyloid-β plaques. In CD-1 mice, it shows moderate clearance and good exposure, and exhibits good central nervous system (CNS) exposure in both mice and rats. EP2 receptor antagonist-3 is applicable for research in Alzheimer's disease.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 10 mg | Inquiry | 10-14 weeks | 10-14 weeks | |
| 50 mg | Inquiry | 10-14 weeks | 10-14 weeks |
| Description | EP2 receptor antagonist-3 is a selective antagonist of the EP2 receptor, with an IC50 of 8 nM determined in the hEP2 SPA assay and an IC50 of 50 nM in the hEP2 cAMP assay. It enhances macrophage-mediated clearance of Amyloid-β plaques. In CD-1 mice, it shows moderate clearance and good exposure, and exhibits good central nervous system (CNS) exposure in both mice and rats. EP2 receptor antagonist-3 is applicable for research in Alzheimer's disease. |
| In vitro | EP2 receptor antagonist-3 (Benzoxazepine 52) is a potent inhibitor of human, rat, and mouse EP2 receptors, demonstrating IC50 values of 0.008 μM, 0.01 μM, and 0.01 μM, respectively, in SPA assays. In cAMP assays, the IC50 values are 0.05 μM, 0.03 μM, and 0.004 μM. Additionally, EP2 receptor antagonist-3 (0.001-3.0 μM, 24 h) shows a dose-dependent enhancement of IC21-mediated Aβ plaque phagocytosis in brain slices from 18-month-old Tg2576 mice. |
| Molecular Weight | 423.87 |
| Formula | C23H19ClFN3O2 |
| Cas No. | 1799626-16-6 |
| Smiles | O=C1C=C(C=CN1)CN2CC3=CC(=CC(Cl)=C3OCC2)N4C=CC=5C=C(F)C=CC54 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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