GSK 256066 Trifluoroacetate

This product is for research use only, not for human use. We do not sell to patients.

For small sizes, please check our retail website as below: www.invivochem.com

Size	Price	Stock
100mg	$950	To Be Confirmed
200mg	$1425	To Be Confirmed
500mg	$2405	To Be Confirmed

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Cat #: V32938 CAS #: 1415560-64-3 Purity ≥ 99%

Description: GSK256066 Trifluoroacetate (GSK256066; GSK-256066), the trifluoroacetic acid salt form of GSK256066, is a novel selective inhibitor of PDE4B (phosphodiesterase 4B) with important biological activity (e.g. inhibiting pulmonary neutrophilia) and thus has the potential to be used for treatment for chronic obstructive pulmonary disease.

References: 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.

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Molecular Weight (MW)	632.61
Molecular Formula	C29H27F3N4O7S
CAS No.	1415560-64-3
SMILES Code	O=C(C1=C(NC2=CC=CC(OC)=C2)C3=CC(S(=O)(C4=CC=CC(C(N(C)C)=O)=C4)=O)=CC(C)=C3N=C1)N
Synonyms	GSK256066; GSK-256066; GSK 256066

Protocol	In Vitro	GSK256066 Trifluoroacetate inhibits tumor necrosis factor α production by lipopolysaccharide (LPS)-stimulated human peripheral blood monocytes with IC50 of 0.01 nM. 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 is an exceptionally high-affinity inhibitor of PDE4 designed for inhaled administration.
Protocol	In Vivo	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.

These protocols are for reference only. InvivoChem does not independently validate these methods.

Preparing Stock Solutions

Solvent volume to be added	Mass (the weight of a compound)
Mother liquor concentration	1mg	5mg	10mg	20mg
1mM	1.5808 mL	7.9038 mL	15.8075 mL	31.6151 mL
5mM	0.3162 mL	1.5808 mL	3.1615 mL	6.3230 mL
10mM	0.1581 mL	0.7904 mL	1.5808 mL	3.1615 mL
20mM	0.0790 mL	0.3952 mL	0.7904 mL	1.5808 mL

The molarity calculator equation

Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)

Mass

Concentration

Volume

Molecular Weight*

The dilution calculator equation

Concentration_(start) × Volume_(start) = Concentration_(final) × Volume_(final)

This equation is commonly abbreviated as: C₁ V₁ = C₂ V₂

Concentration_(start)

Volume_(start)

Concentration_(final)

Volume_(final)

Step One: Enter information below

Dosage mg/kg Average weight of animals g Dosing volume per animal µL Number of animals

Step Two: Enter the in vivo formulation

%DMSO + % + %Tween 80 + %ddH₂O

Calculation Results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in µL DMSO(Master liquid concentration mg/mL) ,Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation: Take µL DMSO master liquid, next add µL PEG300, mix and clarify, next add µL Tween 80,mix and clarify, next add µL ddH₂O,mix and clarify.

Note:

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.