Biological Activity
SB-265610 is a selective, competitive, nonpeptide and allosteric CXCR2 antagonist. SB-265610 blocks rat cytokine-induced neutrophil chemoattractant-1 (CINC-1)-induced calcium mobilization and neutrophil chemotaxis with IC50s of 3.7 nM and 70 nM, respectively[1][2].
In Vitro
In vitro, SB-265610 antagonizes rat cytokine-induced neutrophil chemoattractant-1 (CINC-1)-induced calcium mobilization, IC50 of 3.7 nM, and rat neutrophil chemotaxis in a concentration-dependent manner, IC50 of 70 nM. SB-265610 reduces the antiapoptotic effect of CINC-1 to the levels of those untreated with CINC-1[1].
In Vivo
In vitro, SB-265610 antagonizes rat cytokine-induced neutrophil chemoattractant-1 (CINC-1)-induced calcium mobilization, IC50 of 3.7 nM, and rat neutrophil chemotaxis in a concentration-dependent manner, IC50 of 70 nM. SB-265610 reduces the antiapoptotic effect of CINC-1 to the levels of those untreated with CINC-1[1].
Target
CXCR2
References & source
[1]. Auten RL, et al. Nonpeptide CXCR2 antagonist prevents neutrophil accumulation in hyperoxia-exposed newborn rats. J Pharmacol Exp Ther. 2001 Oct;299(1):90-5.
[2]. Milatovic S, et al. Impaired healing of nitrogen mustard wounds in CXCR2 null mice. Wound Repair Regen. 2003 May-Jun;11(3):213-9.
Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.