Ladarixin sodium

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种新型变构、非竞争性双重 CXCR1/2 抑制剂，可在体外抑制人多形核白细胞 (PMN) 迁移至 CXCL8，IC50 为 0.7 nM。

A novel allosteric, noncompetitive dual CXCR1/2 inhibitor that inhibits human polymorphonuclear leukocyte (PMN) migration to CXCL8 in vitro with IC50 of 0.7 nM; prevents PMN infiltration and tissue damage in several models of IR injury in vivo; abrogates motility and induces apoptosis in cultured cutaneous and uveal melanoma cells and xenografts; also prevents inflammation-mediated damage in MLD-STZ, prevents and reverses diabetes in NOD mice.Diabetes Phase 2 Clinical.

Ladarixin inhibits human polymorphonuclear leukocyte (PMN) migration to CXCL8 (IC50 at 0.7 nM).

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.Ladarixin (10 mg/kg; p.o. once a day for 8 days) reduces pulmonary inflammation and fibrosis induced by bleomycin in mice.Ladarixin (10 mg/kg; p.o. once a day for 3 days) protects mice from cigarette smoke-induced exacerbation of influenza-A infection.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. Animal Model:Mice (cigarette smoke-induced exacerbation of Influenza-A infection model)Dosage:10 mg/kg Administration:P.o. once a day at days 2, 3 and 4 post-infection Result:Significantly attenuated the exacerbation in lethality and respiratory changes noted in CSFlu group.

DF-2156 | DF-2156A

GPCR/G Protein

Chemokine Receptor

Chemokine Receptor

Metabolic Disease

Diabetes

865625-56-5

397.315

C11H11F3NNaO6S2

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (251.69 mM)

CC(C1=CC=C(C=C1)OS(=O)(=O)C(F)(F)F)C(=O)[N-]S(=O)(=O)C.[Na+]

4-((2R)-1-Oxo-1-(methanesulfonamido)propan-2-yl)phenyl trifluoromethanesulfonate sodium salt

(-20℃)

With Ice Pack

≥ 2 years