GSK256066 is an exceptionally high affinity and selective PDE4 inhibitor with an IC50 of 3.2 pM for PDE4B. GSK256066 suppressed tumor necrosis factor ¦Á 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 ¦Ìg/kg). In ferrets, inhaled GSK256066 inhibited LPS-induced pulmonary neutrophilia (ED50=18 ¦Ìg/kg) and no emetic episodes were observed

June 21, 2017

prudect name : GSK256066 is an exceptionally high affinity and selective PDE4 inhibitor with an IC50 of 3.2 pM for PDE4B. GSK256066 suppressed tumor necrosis factor ¦Á 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 ¦Ìg/kg). In ferrets, inhaled GSK256066 inhibited LPS-induced pulmonary neutrophilia (ED50=18 ¦Ìg/kg) and no emetic episodes were observed
GSK256066

Synonyms: CAS NO: 801312-28-7Molecular Formula: C₂₇H₂₆N₄O₅SMolecular Weight: 518.58Purity: 98% minSolubility: In DMSOStorage: −20°C

INNO 206 References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18515689