Biological Activity
Danirixin (GSK1325756) is an orally active, selective CXC chemokine receptor 2 (CXCR2) antagonist with 78-fold lower affinity toward CXCR1 (CXCR2/CXCR1 IC50 = 12.5/977 nM by competitive binding against 0.225 nM [125I] CXCL8). Danirixin blocks agonist-induced neutrophil CD11b expression in vitro (IC50 = 420/890 nM against induction by 10 nM human CXCL1/r at CXCL2 using rat/human whole blood) and prevents lung neutrophils influx in rats in vivo following aerosol lipopolysaccharide or ozone challenge (ED50 = 1.4 and 16 mg/kg, respectively).
