1. Metabolic Enzyme/Protease
  2. Phosphodiesterase (PDE)
  3. GSK256066 Trifluoroacetate

GSK256066 Trifluoroacetate 

Cat. No.: HY-70069 Purity: 99.54%
Handling Instructions

GSK256066 Trifluoroacetate is a selective and high-affinity phosphodiesterase 4 (PDE) inhibitor, with an IC50 of 3.2 pM for PDE4B. GSK256066 Trifluoroacetate is developed for the research of chronic obstructive pulmonary disease.

For research use only. We do not sell to patients.

GSK256066 Trifluoroacetate Chemical Structure

GSK256066 Trifluoroacetate Chemical Structure

CAS No. : 1415560-64-3

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply Now  
Solution
10 mM * 1 mL in DMSO USD 234 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 234 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 168 In-stock
Estimated Time of Arrival: December 31
10 mg USD 300 In-stock
Estimated Time of Arrival: December 31
50 mg USD 864 In-stock
Estimated Time of Arrival: December 31
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Description

GSK256066 Trifluoroacetate is a selective and high-affinity phosphodiesterase 4 (PDE) inhibitor, with an IC50 of 3.2 pM for PDE4B. GSK256066 Trifluoroacetate is developed for the research of chronic obstructive pulmonary disease[1].

IC50 & Target

IC50: 3.2 pM (PDE4B)[1]

In Vitro

GSK256066 Trifluoroacetate is an exceptionally high-affinity inhibitor of PDE4 designed for inhaled administration[1].
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[1].
GSK256066 Trifluoroacetate inhibits tumor necrosis factor α production by lipopolysaccharide (LPS)-stimulated human peripheral blood monocytes with IC50 of 0.01 nM[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.[2].
GSK256066 Trifluoroacetate inhibits LPS-induced pulmonary neutrophilia, and no emetic episodes are observed in ferrets[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Brown Norway rats(180-200 g)[2]
Dosage: 0.3-100 μg/kg
Administration: Intratracheally; 30 minutes before and 6 hours after ovalbumin challenge
Result: Inhibited the increase in eosinophil number in the BAL in a dose-dependent fashion.
Clinical Trial
Molecular Weight

632.61

Formula

C₂₉H₂₇F₃N₄O₇S

CAS No.
Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (79.04 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.5808 mL 7.9038 mL 15.8075 mL
5 mM 0.3162 mL 1.5808 mL 3.1615 mL
10 mM 0.1581 mL 0.7904 mL 1.5808 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 3.25 mg/mL (5.14 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 3.25 mg/mL (5.14 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Product Name:
GSK256066 Trifluoroacetate
Cat. No.:
HY-70069
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