产品
编 号:F154234
分子式:C29H27F3N4O7S
分子量:632.61
产品类型
结构图
CAS No: 1415560-64-3
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产品详情
生物活性:
GSK256066 Trifluoroacetate is a selective and high-affinity phosphodiesterase 4 (PDE) inhibitor, with an IC50 of 3.2 pM for PDE4B. GSK256066 Trifluoroacetate is developed for the research of chronic obstructive pulmonary disease.
体内研究:
GSK256066 Trifluoroacetate (0.3-100 μg/kg; intratracheally) inhibits the eosinophil number increased in the bronchoalveolar lavage (BAL) in a dose-dependent fashion, in lipopolysaccharide (LPS)- and ovalbumin (OVA)-induced acute pulmonary inflammation rat models..GSK256066 Trifluoroacetate inhibits LPS-induced pulmonary neutrophilia, and no emetic episodes are observed in ferrets.Animal Model:Male Brown Norway rats(180-200 g)
Dosage:0.3-100 μg/kg
Administration:Intratracheally; 30 minutes before and 6 hours after ovalbumin challenge
Result:Inhibited the increase in eosinophil number in the BAL in a dose-dependent fashion.
体外研究:
GSK256066 Trifluoroacetate is an exceptionally high-affinity inhibitor of PDE4 designed for inhaled administration. GSK256066 Trifluoroacetate is highly selective for PDE4, with >380,000-fold versus PDE1/2/3/5/6 and >2500-fold against PDE7, and inhibits PDE4 isoforms A-D with equal affinity.GSK256066 Trifluoroacetate inhibits tumor necrosis factor α production by lipopolysaccharide (LPS)-stimulated human peripheral blood monocytes with IC50 of 0.01 nM.