1. Metabolic Enzyme/Protease
  2. Phosphodiesterase (PDE)

GSK256066 

Cat. No.: HY-10469 Purity: 98.46%
SDS Handling Instructions

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.

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GSK256066 Chemical Structure

GSK256066 Chemical Structure

CAS No. : 801312-28-7

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO $171 In-stock
5 mg $150 In-stock
10 mg $275 In-stock
50 mg $800 In-stock
100 mg $1008 In-stock
200 mg   Get quote  
500 mg   Get quote  

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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. IC50 value: 3.2 pM [1] Target: PDE4B 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].

Clinical Trial
NCT Number Sponsor Condition Start Date Phase
NCT00612820 GlaxoSmithKline Rhinitis, Allergic, Seasonal January 2008 Phase 2
NCT00445510 GlaxoSmithKline Asthma June 2006 Phase 2
NCT00612118 GlaxoSmithKline Allergic Rhinitis|Rhinitis, Allergic, Seasonal February 2008 Phase 2
NCT00464568 GlaxoSmithKline Rhinitis, Allergic, Seasonal|Seasonal Allergic Rhinitis|SAR March 2007 Phase 2
NCT00380354 GlaxoSmithKline Asthma|Mild Asthma September 2006 Phase 2
NCT00430157 GlaxoSmithKline Rhinitis, Allergic, Seasonal|Seasonal Allergic Rhinitis January 2007 Phase 2
NCT00377728 GlaxoSmithKline Rhinitis, Allergic, Seasonal|Seasonal Allergic Rhinitis March 2006 Phase 2
NCT00549679 GlaxoSmithKline Pulmonary Disease, Chronic Obstructive October 2007 Phase 2
NCT00515268 GlaxoSmithKline Pulmonary Disease, Chronic Obstructive|Healthy Subjects September 2007 Phase 1
NCT00549744 GlaxoSmithKline Asthma November 16, 2007 Phase 2
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References
Molecular Weight

518.58

Formula

C₂₇H₂₆N₄O₅S

CAS No.

801312-28-7

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 5.2 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Product Name:
GSK256066
Cat. No.:
HY-10469
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