In vitro activity: Danirixin (formerly known as GSK1325756) is a a potent small molecule CXCR2 antagonist being developed as a potential anti-inflammatory drug. It is a selective, high-affinity and reversible CXCR2 antagonist with IC50 of 12.5 nM for CXCL8. The dose-dependent inhibition of agonist-induced neutrophil activation following single and repeated once daily oral administration of danirixin suggests that this CXCR2 antagonist may have benefit in neutrophil-predominant inflammatory diseases. Excessive neutrophil presence and activation is important in a number of acute and chronic inflammatory diseases. The CXCR2 chemokine receptor is important in controlling the extravasation and activation of neutrophils. Selective antagonism of the CXCR2 receptor is a potential approach to reducing neutrophil migration and activation.

Kinase Assay: It is a selective, high-affinity and reversible CXCR2 antagonist with IC50 of 12.5 nM for CXCL8.

Cell Assay: