NE 52-QQ57

NE 52-QQ57 is a selective, and orally available GPR4 antagonist with an IC50 of 70 nM[1]. Anti-inflammatory activities[1].

NE 52-QQ57 (compound 13) shows a significant anti-inflammatory effect in the rat antigen induced arthritis model after oral administration at 30 mg/kg bid for 20 days[1].NE 52-QQ57 (30 mg/kg bid po for 4 days) also prevents angiogenesis in the mouse chamber model as well as pain as demonstrated in the rat complete Freund's adjuvant model[1].|| Animal Model:|Female FVB mice (8-10 weeks)[1]|Dosage:|30 mg/kg bid po|Administration:|Oral, 4 days, bid|Result:|Treatment with GPR4 antagonist 3 at 30 mg/ kg po bid starting on day 0, the day of the chamber implantation, showS a statistically significant reduction (46.8 ± 10.6%) of tissue growth by day 4. The blood levels of 13 on day 4 at 2 and 16 h after compound application in this model are 9.03 ± 2.87 and 0.09 ± 0.06 μM[1].|| Animal Model:|Male Wistar Han rats[1]|Dosage:|3, 10, and 30 mg/kg|Administration:|Oral, 20 days, bid|Result:|GPR4 antagonist 3 displays not only higher exposures in the rat AIA but also lower plasma protein binding in rat (95%)[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.