TG11-77 is a brain-permeable antagonist of the prostaglandin E2 (PGE2) receptor subtype EP2 (KB = 9.7 nM).1 It is selective for EP2 over DP1, EP4, and IP receptors (KBs = 7,320, 5,300, and >10,000 nM, respectively). TG11-77 (0.3 and 1 μM) inhibits the expression of genes encoding COX-2, IL-1β, and IL-6 induced by LPS and the EP2 receptor agonist ONO-AE1-259-01 in mouse BV-2 microglia expressing human EP2 receptors.
1.Amaradhi, R., Banik, A., Mohammed, S., et al.Potent, selective, water soluble, brain-permeable EP2 receptor antagonist for use in central nervous system disease modelsJ. Med. Chem.63(3)1032-1050(2020)