EP2 receptor antagonist-3 

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 shows moderate clearance and good exposure in CD-1 mice and good CNS exposure in mice and rats. EP2 receptor antagonist-3 can be used for the study of alzheimer’s diseases^[1].

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.

423.87

C₂₃H₁₉ClFN₃O₂

1799626-16-6

O=C1C=C(CN2CC3=CC(N4C=CC5=C4C=CC(F)=C5)=CC(Cl)=C3OCC2)C=CN1

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Fox BM, et al. A selective prostaglandin E2 receptor subtype 2 (EP2) antagonist increases the macrophage-mediated clearance of amyloid-beta plaques. J Med Chem. 2015 Jul 9;58(13):5256-73.  [Content Brief]