5-Pyrimidinecarboxamide, 2-[(4,6-dimethyl-2-pyridinyl)amino]-N-[2-(2-methyl-1H-indol-3-yl)ethyl]-, hydrochloride (1:1)

TG11-77 is a brain-permeable antagonist of the prostaglandin E₂ (PGE₂) receptor subtype EP₂ (K_B = 9.7 nM).¹ It is selective for EP₂ over DP₁, EP₄, and IP receptors (K_Bs = 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 models J. Med. Chem. 63(3),1032-1050(2020).