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GSK256066 Trifluoroacetate

CAS No. : 1415560-64-3

MCE 国际站：GSK256066 Trifluoroacetate

产品活性：GSK256066 Trifluoroacetate 是一种选择性、高亲和力的 PDE 抑制剂，抑制 PDE4B 的 IC₅₀ 值为 3.2 pM。GSK256066 Trifluoroacetate 被开发用于慢性阻塞性肺病的研究。

研究领域：Metabolic Enzyme/Protease

作用靶点：Phosphodiesterase (PDE)

In Vitro: 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.

In Vivo: 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.

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