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GSK256066

Name: GSK256066
Brand: Selleck Chemicals
SKU: S2620
Rating: 5 (1 reviews)

Catalog No.S2620

For research use only.

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.

CAS No. 801312-28-7

Selleck's GSK256066 has been cited by 1 Publication

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PDE Signaling Pathway Map

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 (from reference)

Animal Research:^[1]	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.

References

Solubility (25°C)

In vitro


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. Click to purchase: Tween 80	30 mg/mL

Chemical Information

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

Download GSK256066 SDF

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

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Dilution Calculator Molecular Weight Calculator

Clinical Trial Information

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

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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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