GSK 256066 Trifluoroacetate

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效的选择性 PDE4 抑制剂，对 PDE4B、A、C 和 D 的 pIC50 分别为 11.5、11.3、11.4 和 11.9。

A potent, selective PDE4 inhibitor with pIC50 of 11.5, 11.3, 11.4, and 11.9 for PDE4B, A, C, and D, respectively; displays >380,000-fold selectivity over PDE1/23/5/6/7; inhibits TNFα production by lLPS-stimulated human peripheral blood monocytes with IC50 of 0.01 nM; inhibites LPS-induced pulmonary neutrophilia with ED50 of 1.1 ug/kg (aqueous suspension) and 2.9 ug/kg (dry powder formulation) in rats.COPD Phase 2 Discontinued.

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.

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.

GSK-256066 | GSK256066 (2,2,2-trifluoroacetic acid)

Angiogenesis

PDE

PDE

Inflammation/Immunology

COPD

1415560-64-3

632.6075

C29H27F3N4O7S

>98% (HPLC)

10 mM in DMSO

CC1=CC(=CC2=C(C(=CN=C12)C(=O)N)NC3=CC(=CC=C3)OC)S(=O)(=O)C4=CC=CC(=C4)C(=O)N(C)C.C(=O)(C(F)(F)F)O

3-Quinolinecarboxamide, 6-[[3-[(dimethylamino)carbonyl]phenyl]sulfonyl]-4-[(3-methoxyphenyl)amino]-8-methyl-, 2,2,2-trifluoroacetate (1:1)

(-20℃)

With Ice Pack

≥ 2 years