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

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]	- Collapse 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)

References

Solubility (25°C)

In vitro	DMSO	5 mg/mL (9.64 mM)
	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 Download GSK256066 SDF

Molecular Weight	518.58
Formula	C₂₇H₂₆N₄O₅S
CAS No.	801312-28-7
Storage	3 years -20°C powder
Storage	2 years -80°C in solvent
Synonyms	N/A

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Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2019-10-14)

NCT Number	Recruitment	interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
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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