Cabozantinib/XL184

溶解度:Unknown

储存条件:at -20℃ 2 years

生物活性

GSK256066 is an exceptionally high affinity and selective PDE4 inhibitor with an IC50 of 3.2 pM for PDE4B. GSK256066 suppressed tumor necrosis factor α production by lipopolysaccharide (LPS)-stimulated human peripheral blood monocytes with 0.01 nM IC50 (compared with IC50 values of 5, 22, and 389 nM for roflumilast, tofimilast, and cilomilast, respectively) and by LPS-stimulated whole blood with 126 pM IC50. GSK256066 also inhibited LPS-induced increases in exhaled nitric oxide (ED50=35 µg/kg). In addition, GSK256066 prevented pulmonary eosinophilia in rats exposed to ovalbumin (ED50=0.4 μg/kg). In ferrets, inhaled GSK256066 inhibited LPS-induced pulmonary neutrophilia (ED50=18 μg/kg) and no emetic episodes were observed. ^[1][2]

参考文献

[1] Nials AT et al. J Pharmacol Exp Ther. 2011 Apr; 337(1):137-44.

[2] Singh D et al. Respir Res. 2010 Mar 1; 11:26.