GPR4 antagonist 3

GPR4 antagonist 3 is a selective, and orally available GPR4 antagonist with an IC50 of 70 nM[1]. Anti-inflammatory activities[1].

Signaling Pathways >> Others >> Others

Research Areas >> Inflammation/Immunology

IC50: 70 nM (GPR4)[1].

GPR4 antagonist 3 shows a significant anti-inflammatory effect in the rat antigen induced arthritis model after oral administration at 30 mg/kg bid[1].GPR4 antagonist 3 also prevents angiogenesis in the mouse chamber model as well as pain as demonstrated in the rat complete Freund’s adjuvant model[1].

[1]. Velcicky J, et al. Development of Selective, Orally Active GPR4 Antagonists with Modulatory Effects on Nociception, Inflammation, and Angiogenesis. J Med Chem. 2017 May 11;60(9):3672-3683.