Description
TG11-77 is a brain-permeable antagonist of the prostaglandin E
2 (PGE
2) receptor subtype EP
2 (K
B = 9.7 nM).
1 It is selective for EP
2 over DP
1, EP
4, 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 EP
2 receptor agonist ONO-AE1-259-01 in mouse BV-2 microglia expressing human EP
2 receptors.
References
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).
![5-Pyrimidinecarboxamide, 2-[(4,6-dimethyl-2-pyridinyl)amino]-N-[2-(2-methyl-1H-indol-3-yl)ethyl]-, hydrochloride (1:1) Structure](https://www.chemicalbook.com/CAS/20211123/GIF/2550393-38-7.gif)