SB-265610 是竞争性非肽变构CXCR2选择性拮抗剂,可阻断大鼠 CINC-1 诱导的钙动员和中性粒细胞趋化性,IC50分别为 3.7 和 70 nM。
产品描述
SB-265610 is a nonpeptide and allosteric CXCR2 antagonist. SB-265610 blocks rat cytokine-induced neutrophil chemoattractant-1 (CINC-1)-induced calcium mobilization and neutrophil chemotaxis (IC50s: 3.7 nM and 70 nM, respectively).
体外活性
SB-265610 decreases the antiapoptotic effect of CINC-1 to the levels of those untreated with CINC-1. 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) [1].
体内活性
SB-265610 (100 mg/kg/day;p.o; daily; for 5 days; CXCR2 wild type mice) treatment markedly delays healing parameters in CXCR2 wild type mice during the wound repair process[2].
Cas No.
211096-49-0
分子式
C14H9BrN6O
分子量
357.17
别名
GSK-CXCR2
储存和溶解度
DMSO:66 mg/mL (184.79 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years