Home Metabolism PDE inhibitor GSK256066 For research use only.

GSK256066

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.

GSK256066 Chemical Structure

GSK256066 Chemical Structure

CAS: 801312-28-7

Selleck's GSK256066 has been cited by 2 publications

Purity & Quality Control

Batch: S262001 4-Methylpyridine] 11 mg/mL] true] DMSO] Insoluble] false] Water] Insoluble] false Purity: 99.31%
99.31

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Signaling Pathway

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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
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
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]
Animal Research Animal Models Male CD rats
Dosages 0.1–100 μg/kg
Administration Administered intratracheally as an aqueous suspension or a dry powder 2 h before LPS challenge.
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
GlaxoSmithKline
 November 16 2007 Phase 2
NCT00549679 Completed
Pulmonary Disease Chronic Obstructive
GlaxoSmithKline
 October 4 2007 Phase 2
NCT00515268 Completed
Pulmonary Disease Chronic Obstructive
GlaxoSmithKline
 September 27 2007 Phase 1
NCT00464568 Completed
Rhinitis Allergic Seasonal
GlaxoSmithKline
 March 28 2007 Phase 2

Chemical Information & Solubility

Molecular Weight 518.58 Formula

C27H26N4O5S
CAS No. 801312-28-7 SDF Download GSK256066 SDF
Smiles CC1=CC(=CC2=C(C(=CN=C12)C(=O)N)NC3=CC(=CC=C3)OC)S(=O)(=O)C4=CC=CC(=C4)C(=O)N(C)C
Storage (From the date of receipt)

In vitro
Batch:

4-Methylpyridine : 11 mg/mL

DMSO : Insoluble ( Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble


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In vivo
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Tech Support

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.

Handling Instructions

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