Elubrixintosylate(SB-656933tosylate)是一种有效，选择性，竞争性，可逆和具有口服活性的CXCR2拮抗剂和IL-8受体拮抗剂。Elubrixintosylate抑制中性粒细胞CD11b上调(IC50为260.7nM)和形状改变(IC50为310.5nM)。Elubrixintosylate可用于炎症性疾病的研究，例如炎症性肠病和气道炎症。
货号:ajcx30580
CAS:960495-43-6
分子式:C24H25Cl2FN4O7S2
分子量：635.51
溶解度:DMSO: 125 mg/mL (196.69 mM)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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

Elubrixin has an inhibitory effect on neutrophils in a dose-dependent fashion[1].

[1]. Mozaffari S, et al. Inflammatory bowel disease therapies discontinued between 2009 and 2014. Expert Opin Investig Drugs. 2015;24(7):949-56. [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. [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.