GSK256066
Catalog No.S2620

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. | ||
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Targets |
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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] |
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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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Solubility (25°C)
In vitro | DMSO | 5 mg/mL (9.64 mM) |
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Water | Insoluble | |
Ethanol | Insoluble | |
In vivo | Add solvents to the product individually and in order(Data is from Selleck tests instead of citations): 30% propylene glycol, 5% Tween 80, 65% D5W For best results, use promptly after mixing. |
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 |
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Formula | C27H26N4O5S |
CAS No. | 801312-28-7 |
Storage | powder |
in solvent | |
Synonyms | N/A |
Bio Calculators
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Clinical Trial Information
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
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NCT00612118 | Completed | Drug: GSK256066|Drug: azelastine hydrochloride | Allergic Rhinitis|Rhinitis Allergic Seasonal | GlaxoSmithKline | February 2008 | Phase 2 |
NCT00612820 | Completed | Drug: GSK256066|Drug: fluticasone propionate | Rhinitis Allergic Seasonal | GlaxoSmithKline | January 2008 | Phase 2 |
NCT00549744 | Completed | Drug: GSK256066 | Asthma | GlaxoSmithKline | November 16 2007 | Phase 2 |
NCT00549679 | Completed | Drug: GSK256066|Drug: Placebo | Pulmonary Disease Chronic Obstructive | GlaxoSmithKline | October 4 2007 | Phase 2 |
NCT00515268 | Completed | Drug: GSK256066|Drug: Placebo | Pulmonary Disease Chronic Obstructive | GlaxoSmithKline | September 27 2007 | Phase 1 |
NCT00464568 | Completed | Drug: GSK256066 | Rhinitis Allergic Seasonal | GlaxoSmithKline | March 28 2007 | Phase 2 |
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