NE 52-QQ57 |
Catalog No.GC31906 |
NE 52-QQ57 est un antagoniste GPR4 sélectif et disponible par voie orale avec une IC50 de 70 nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1401728-56-0
Sample solution is provided at 25 µL, 10mM.
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.
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