688763-65-7

Elubrixin, also known as SB-656933 or SB-656933-AAF, is a interleukin 8 inhibitor and CXCR2 selective antagonist, which is potentially useful for Inflammatory bowel disease therapies. Elubrixin inhibits ex vivo neutrophil activation and ozone-induced airway inflammation in humans. demonstrates dose-dependent effects on neutrophil activation and recruitment within a well-tolerated dose range. SB-656933 may be an effective agent in neutrophil-predominant diseases.

Elubrixin (SB-656933) hydrochloride is a potent, selective, competitive, reversible and orally active CXCR2 antagonist and an IL-8 receptor antagonist. Elubrixin hydrochloride inhibits neutrophil CD11b upregulation (IC50 of 260.7 nM) and shape change (IC50 of 310.5 nM). Elubrixin hydrochloride has the potential for inflammatory diseases research, such as inflammatory bowel disease and airway inflammation[1][2][3].

[1] Mozaffari S, et al. Inflammatory bowel disease therapies discontinued between 2009 and 2014. Expert Opin Investig Drugs. 2015;24(7):949-56. DOI:10.1517/13543784.2015.1035432
[2] Lazaar AL, et al. SB-656933, a novel CXCR2 selective antagonist, inhibits ex vivo neutrophil activation and ozone-induced airway inflammation in humans. Br J Clin Pharmacol. 2011 Aug;72(2):282-93. DOI:10.1111/j.1365-2125.2011.03968.x
[3] Nicholson GC, et al. A novel flow cytometric assay of human whole blood neutrophil and monocyte CD11b levels: upregulation by chemokines is related to receptor expression, comparison with neutrophil shape change, and effects of a chemokine receptor (CXCR2) antagonist. Pulm Pharmacol Ther. 2007;20(1):52-9. DOI:10.1016/j.pupt.2005.11.009