R-406

溶解度:Unknown

储存条件:at -20℃ 2 years

生物活性

R406 is an orally available spleen tyrosine kinase inhibitor with an IC50 of 41 nM. R406 blocked Syk-dependent FcR-mediated activation of monocytes/macrophages and neutrophils and BCR-mediated activation of B lymphocytes. R406 has shown efficacy in a number of animal models of immune disorders. R406 inhibited airway hyperresponsiveness (AHR) and airway inflammation in mice, at least in part through alteration of mast cell and dendritic cell functions. Similarly, R406 treatment ameliorated joint inflammation in a number of rodent models of rheumatoid arthritis and also blocked JNK-mediated gene expression in human synoviocytes, suggesting a possible role in the treatment of rheumatoid arthritis

参考文献

[1] Zhu Y et al. Toxicol Appl Pharmacol. 2007 Jun 15;221(3):268-77. [2] Sweeny DJ et al. Xenobiotica. 2010 Jun;40(6):415-23.