Free shipping on all orders over $ 500

GSK256066

Cat. No. M1728
GSK256066 Structure
Size Price Availability Quantity
10mg USD 280 In stock
50mg USD 780 In stock
100mg USD 1020 In stock
Bulk Inquiry?

Quality Control
Biological Activity

GSK256066 is a selective phosphodiesterase 4 (PDE4)inhibitor with an IC50 of 3.2  pM. Oral phosphodiesterase (PDE)4 inhibitors have demonstrated clinical efficacy in chronic obstructive pulmonary disease and asthma. Preclinical andclinical investigation of inhaled PDE4 inhibitors is ongoing. GSK256066 may have an improved therapeutic index compared with oral PDE4 inhibitors, e.g., cilomilast and roflumilast.GSK256066 demonstrates potent and long-lasting anti-inflammatory effects in animal models of pulmonary inflammation and does not induce emetic episodes in ferrets. GSK256066 has potential as an inhaled therapeutic for the treatment of asthma and chronic obstructive pulmonary disease.

Protocol
Cell Experiment
Cell lines PBMCs cells line
Preparation method Compound Preparation for In Vitro Assays.
Dilution series for pIC50 determinations generally comprised eight successive 3-fold dilutions in DMSO. Low-volume additions (0.5-2.0 μl) to assays were carried out using a Biomek Fx liquid-handling robot (Beckman Coulter, Fullerton, CA).Percentages of inhibition values were generated relative to uninhibited controls. Values for pIC50 were determined from concentration-response curves by nonlinear least-squares curve fitting, in general using a four-parameter logistic equation in Activity Base (IDBS, Guildford, Surrey, UK).
Concentrations 0~10 μM
Incubation time 72 h
Animal Experiment
Animal models LPS-induced pulmonary neutrophilia in rats model
Formulation 0.2% Tween 80 in normal saline
Dosages 0.1-100 μg/kg
Administration intratracheally
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 518.58
Formula C27H26N4O5S
CAS Number 801312-28-7
Purity 98.53%
Solubility DMSO
Storage at -20°C
References

In vivo characterization of GSK256066, a high-affinity inhaled phosphodiesterase 4 inhibitor.
Nials et al. J Pharmacol Exp Ther. 2011 Apr;337(1):137-44. PMID: 21205924.

GSK256066, an exceptionally high-affinity and selective inhibitor of phosphodiesterase 4 suitable for administration by inhalation: in vitro, kinetic, and in vivo characterization.
Tralau-Stewart et al. J Pharmacol Exp Ther. 2011 Apr;337(1):145-54. PMID: 21205923.

The inhaled phosphodiesterase 4 inhibitor GSK256066 reduces allergen challenge responses in asthma.
Singh et al. Respir Res. 2010 Mar 1;11:26. PMID: 20193079.

Related PDE Products
E6005

RVT-501 (E6005) is a selective phosphodiesterase 4 (PDE4PDE4) inhibitor with an IC50 of 2.8 nM.

Vardenafil HCl

Vardenafil Hcl is a PDE5 inhibitor used for treating erectile dysfunction.

Udenafil

Udenafil(DA8159) is a PDE5 inhibitor used in urology to treat erectile dysfunction.

Theophylline

Theophylline is a methylated xanthine derivative; competitive nonselective phosphodiesterase inhibitor and nonselective adenosine receptor antagonist.

Sildenafil Mesylate

Sildenafil Mesylate is a mesylate form of Sildenafil, an inhibitor of Phosphodiesterase 5.

  Catalog
Abmole Inhibitor Catalog 2017




Keywords: GSK256066 supplier, PDE, inhibitors

Contact Us

Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2017 AbMole BioScience. All Rights Reserved.