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/rat 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).
International immunopharmacology, 95, 107153-107153 (2021-03-08)
Breast cancer is the most frequent cancer among females and the second most common cause of cancer deaths worldwide. Tumor-associated macrophages (TAMs) are the most abundant immune cell population in the tumor microenvironment, including breast cancer. Breast cancer stem cells
Danirixin: A Reversible and Selective Antagonist of the CXC Chemokine Receptor 2
Journal of Pharmacology and Experimental Therapeutics, 362(2), 338-346 (2017)
CXCL-8-dependent and -independent neutrophil activation in COPD: experiences from a pilot study of the CXCR2 antagonist danirixin.
ERJ open research, 6(4), 00583-2020 (2020)
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