Bioactivity | 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]. | ||||||||||||
Invitro | Ladarixin inhibits human polymorphonuclear leukocyte (PMN) migration to CXCL8 (IC50 at 0.7 nM)[2]. | ||||||||||||
In Vivo | 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]. Animal Model: | ||||||||||||
Name | Ladarixin | ||||||||||||
CAS | 849776-05-2 | ||||||||||||
Formula | C11H12F3NO6S2 | ||||||||||||
Molar Mass | 375.34 | ||||||||||||
Appearance | Solid | ||||||||||||
Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
Storage |
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Reference | [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 |