SB225002

SB225002的生物活性

SB225002 is a potent and selective non-peptide inhibitor of CXCR2 with IC50 of 22 nM; >150-fold selectivity over CXCR1 and four other 7-TMRs.
IC50 value: 22 nM(inhibition of 125I-IL-8 binding to CXCR2) [1]
Target: CXCR2 inhibitor
in vitro: SB 225002 potently inhibited human and rabbit neutrophil chemotaxis induced by both IL-8 and GROalpha [1]. SB-265610 antagonizes rat cytokine-induced neutrophil chemoattractant-1 (CINC-1)-induced calcium mobilization, IC50 = 3.7 nM, and rat neutrophil chemotaxis in a concentration-dependent manner, IC50 = 70 nM [2].
in vivo: SB 225002 selectively blocked IL-8-induced neutrophil margination in rabbits [1]. Newborn rats exposed to 95% O2 for 8 days had increased lung neutrophil content. Injection with 1 to 3 mg/kg SB-265610 on days 3 to 5 reduced hyperoxia-induced neutrophil accumulation in bronchoalveolar lavage and whole lung myeloperoxidase accumulation at the highest doses [2]. i.p. treatment with SB225002 significantly attenuated the increase in MPO activity or the elevation of IL-1beta, TNFalpha or KC levels following carrageenan injection [3].