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GSK256066 Trifluoroacetate

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GSK256066 Trifluoroacetate

Catalog No. T11483Cas No. 1415560-64-3

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.

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Pack Size	Price	Availability
2 mg	$78	5 days
50 mg	$717	1-2 weeks
100 mg	$995	1-2 weeks

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Product Introduction

Bioactivity

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)

Chemical Properties

Molecular Weight	632.61
Formula	C29H27F3N4O7S
Cas No.	1415560-64-3

Storage & Solubility Information

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

	1mg	5mg	10mg	50mg
1 mM	1.5808 mL	7.9038 mL	15.8075 mL	79.0376 mL
5 mM	0.3162 mL	1.5808 mL	3.1615 mL	15.8075 mL
10 mM	0.1581 mL	0.7904 mL	1.5808 mL	7.9038 mL
20 mM	0.0790 mL	0.3952 mL	0.7904 mL	3.9519 mL
50 mM	0.0316 mL	0.1581 mL	0.3162 mL	1.5808 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:

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A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent

DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.

Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O TargetMol | reagent

mix well and clarify

Dose Conversion

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Tech Support

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