| Name | GSK256066 Trifluoroacetate |
| 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. |
| 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. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween-80+45% Saline : 2.5 mg/mL (3.95 mM), Sonication is recommended. DMSO : 50 mg/mL (79.04 mM), Sonication is recommended.
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| Keywords | PDE4B | GSK-256066 Trifluoroacetate | GSK256066 Trifluoroacetate | GSK-256066 | GSK256066 | GSK 256066 | 2,2,2-trifluoroacetic acid |
| Inhibitors Related | Balipodect | Theophylline monohydrate | D(+)-Raffinose pentahydrate | Theobromine | Apremilast | Isoprenaline hydrochloride | Indomethacin | Icariin | Theophylline | Vardenafil hydrochloride | Sildenafil citrate | Doxofylline |