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Pack Size | Price | Availability | Quantity |
---|---|---|---|
2 mg | $78 | 5 days | |
50 mg | $717 | 1-2 weeks | |
100 mg | $995 | 1-2 weeks |
Description | GSK 256066 Trifluoroacetate is a selective and high-affinity phosphodiesterase 4 (PDE) inhibitor (IC50: 3.2 pM for PDE4B). It can be used for the treatment of chronic obstructive pulmonary disease. |
Targets&IC50 | PDE4B:3.2 pM |
In vitro | GSK 256066 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.?GSK 256066 Trifluoroacetate inhibits tumor necrosis factor α production by lipopolysaccharide (LPS)-stimulated human peripheral blood monocytes with IC50 of 0.01 nM.GSK 256066 Trifluoroacetate ?is an exceptionally high-affinity inhibitor of PDE4 designed for inhaled administration. |
In vivo | GSK 256066 Trifluoroacetate inhibits LPS-induced pulmonary neutrophilia, and no emetic episodes are observed in ferrets.GSK 256066 Trifluoroacetate (GSK256066 2,2,2-trifluoroacetic acid; 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. |
Alias | GSK 256066 Trifluoroacetate, GSK256066 (2,2,2-trifluoroacetic acid) |
Molecular Weight | 632.61 |
Formula | C29H27F3N4O7S |
Cas No. | 1415560-64-3 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
Solubility Information | DMSO: 50 mg/mL (79.04 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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