Ladarixin (DF 2156A free base) 是一种具有口服活性的，非竞争性的 CXCR1 和 CXCR2 的变构抑制剂。Ladarixin 可用于 COPD 和哮喘的研究。
Ladarixin (DF 2156A free base) is an orally active, allosteric non-competitive and dual CXCR1 and CXCR2 antagonist. Ladarixin can be used for the research of COPD and asthma[1].
Ladarixin inhibits human polymorphonuclear leukocyte (PMN) migration to CXCL8 (IC50 at 0.7 nM)[2].
Ladarixin (10 mg/kg; p.o. once a day) reduces allergic airway inflammation in a model of single OVA exposure. Ladarixin reduces allergic airway inflammation, remodeling, and bronchial hyperreactivity in a model of chronic OVA exposure[1].Ladarixin (10 mg/kg; p.o. once a day for 8 days) reduces pulmonary inflammation and fibrosis induced by bleomycin in mice[1].Ladarixin (10 mg/kg; p.o. once a day for 3 days) protects mice from cigarette smoke-induced exacerbation of influenza-A infection[1].Ladarixin is also effective in decreasing CXCL8-induced polymorphonuclear leukocyte infiltration in several animal models without a significant dose-related reduction in systemic neutrophil counts[2].
[1]. Matheus Silverio Mattos, et al. CXCR1 and CXCR2 Inhibition by Ladarixin Improves Neutrophil-Dependent Airway Inflammation in Mice. Front Immunol. 2020 Oct 2;11:566953.
[2]. Daria Marley Kemp, et al. Ladarixin, a dual CXCR1/2 inhibitor, attenuates experimental melanomas harboring different molecular defects by affecting malignant cells and tumor microenvironment. Oncotarget. 2017 Feb 28;8(9):14428-14442
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