GSK256066

Catalog No.S2620

GSK256066 Chemical Structure

Molecular Weight(MW): 518.58

GSK256066 is a selective PDE4B(equal affinity to isoforms A-D) inhibitor with IC50 of 3.2 pM, >380,000-fold selectivity versus PDE1/2/3/5/6 and >2500-fold selectivity against PDE4B versus PDE7.Phase 2.

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Biological Activity

Description GSK256066 is a selective PDE4B(equal affinity to isoforms A-D) inhibitor with IC50 of 3.2 pM, >380,000-fold selectivity versus PDE1/2/3/5/6 and >2500-fold selectivity against PDE4B versus PDE7.Phase 2.
Targets
PDE4B [1]
3.2 pM
In vitro

GSK256066 is a slow and tight binding inhibitor of PDE4B with apparent IC50 of 3.2 pM. GSK256066 is an extremely potent inhibitor of LPS-stimulated TNFα production in PBMCs with pIC50 of 11.0 and IC50 of 10 pM and human whole-blood cultures with pIC50 of 9.90 and IC50 of 126 pM. GSK256066 is highly selective for PDE4 (>3.8 × 105-fold versus PDE1, PDE2, PDE3, PDE5, and PDE6 and >2.5 × 103-fold against PDE7). GSK256066 inhibits PDE4 isoforms A-D with equal affinity. [1]

In vivo GSK256066 inhibits the LPS-induced pulmonary neutrophilia with an ED50 of 1.1 μg/kg, achieving maximal inhibition of 72% at 30 μg/kg when given in the aqueous suspension. GSK256066 inhibits the LPS-induced pulmonary neutrophilia with ED50 of 2.9 μg/kg, achieving maximal inhibition of 62% when given in the dry powder formulation. GSK256066 shows a moderate plasma clearance of 39 ml/min/kg, a moderate volume of distribution of 0.8 L/kg, and a relatively short half-life of 1.1 hour in the male CD rat. [1] GSK256066 sustains at a high lung concentration of 2.6 μg/g after intra-tracheal administration as an aqueous suspension at a dose of 30 μg/kg in rats. [2] GSK256066 (10 μg/kg) is administered intratracheally at different times (2, 6, 12, 18, 24, and 36 hours) before LPS administration, inhibiting LPS-Induced Pulmonary Neutrophilia in rat lipopolysaccharide (LPS)-induced models of acute pulmonary inflammation. GSK256066 (0.3–100 μg/kg) inhibits LPS-induced increases in exhaled nitric oxide with ED50 of 35 μg/kg in rat. GSK256066 (10 μg/kg) is administered half a hour before OVA administration in rat, inhibiting OVA-induced pulmonary eosinophilia with ED50 of 0.4 μg/kg. GSK256066 administered intratracheally as a dry powder blended in respiratory-grade lactose at doses of 3 to 100 μg/kg 2 hours before inhaled LPS challenge in ferrets, inhibiting LPS-induced pulmonary neutrophilia with ED50 of 18 μg/kg without inducing emetic episodes. [3]

Protocol

Animal Research:[1]
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  • Animal Models: Male CD rats
  • Formulation: Sterile 0.9% sodium chloride solution
  • Dosages: 0.1–100 μg/kg
  • Administration: Administered intratracheally as an aqueous suspension or a dry powder 2 h before LPS challenge.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 5 mg/mL (9.64 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents individually and in order:
30% propylene glycol, 5% Tween 80, 65% D5W
30 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 518.58
Formula

C27H26N4O5S

CAS No. 801312-28-7
Storage powder
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00612118 Completed Allergic Rhinitis|Rhinitis, Allergic, Seasonal GlaxoSmithKline February 2008 Phase 2
NCT00612820 Completed Rhinitis, Allergic, Seasonal GlaxoSmithKline January 2008 Phase 2
NCT00549744 Completed Asthma|Mild Asthma GlaxoSmithKline November 2007 Phase 2
NCT00549679 Completed Pulmonary Disease, Chronic Obstructive GlaxoSmithKline October 2007 Phase 2
NCT00515268 Completed Pulmonary Disease, Chronic Obstructive|Healthy Subjects GlaxoSmithKline September 2007 Phase 1
NCT00464568 Completed Rhinitis, Allergic, Seasonal|Seasonal Allergic Rhinitis|SAR GlaxoSmithKline March 2007 Phase 2

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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PDE Signaling Pathway Map

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