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GSK256066 Trifluoroacetate

Catalog No. T11483 CAS 1415560-64-3

Synonyms: GSK 256066 Trifluoroacetate, GSK256066 (2,2,2-trifluoroacetic acid)

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.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

GSK256066 Trifluoroacetate Chemical Structure

GSK256066 Trifluoroacetate, CAS 1415560-64-3

Pack Size	Availability	Price/USD
2 mg	5 days	$ 78.00
50 mg	8-10 weeks	$ 717.00
100 mg	8-10 weeks	$ 995.00

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Biological Description

Chemical Properties

Storage & Solubility Information

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.

Synonyms	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

Solubility Information

DMSO: 50 mg/mL (79.04 mM), Sonication is recommended.

References and Literature

1. Tralau-Stewart CJ, et al. GSK256066, an exceptionally high-affinity and selective inhibitor of phosphodiesterase 4 suitable for administration by inhalation: in vitro, kinetic, and in vivo characterization. J Pharmacol Exp Ther, 2011, 337(1), 145-154. 2. Nials AT, et al. In vivo characterization of GSK256066, a high-affinity inhaled phosphodiesterase 4 inhibitor. J Pharmacol Exp Ther, 2011, 337(1), 137-144.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

GSK256066 Trifluoroacetate 1415560-64-3 Metabolism PDE GSK256066 GSK 256066 Trifluoroacetate 2,2,2-trifluoroacetic acid GSK-256066 GSK-256066 Trifluoroacetate GSK256066 (2,2,2-trifluoroacetic acid) GSK 256066 inhibitor inhibit

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