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Description

A potent and selective antagonist of G-protein coupled receptor CXCR2 (IL-8RB, IC50 = 22 nM for the inhibition of 125I-IL-8 binding to CXCR2). Inhibits human and rabbit neutrophil chemotaxis induced by both IL-8 and GROalpha in vitro and selectively blocks IL-8-induced neutrophil margination in rabbits. Reduces presenilin expression, inhibits gamma-secretase activity, and blocks Abeta40/42 production and notch processing, further, demonstrates in vivo efficacy in mouse models., A potent, selective, and competitive antagonist of the G-protein coupled receptor CXCR2 (IL-8RB, IC50 = 22 nM for the inhibition of 125I-IL-8 binding to CXCR2). Shows ~150-fold selectivity over CXCR1. Inhibits human and rabbit neutrophil chemotaxis induced by both IL-8 and GROalpha in vitro and in vivo selectively blocks IL-8-induced neutrophil margination in rabbits. Reduces presenilin expression, inhibits gamma-secretase activity, and blocks Abeta40/42 production and notch processing, further, demonstrates in vivo efficacy in mouse models.