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GSK256066

Catalog No. T6054 CAS 801312-28-7

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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GSK256066, CAS 801312-28-7

Pack Size	Availability	Price/USD
1 mg	In stock	$ 33.00
2 mg	In stock	$ 47.00
5 mg	In stock	$ 76.00
10 mg	In stock	$ 128.00
25 mg	In stock	$ 263.00
50 mg	In stock	$ 428.00
1 mL * 10 mM (in DMSO)	In stock	$ 87.00

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Purity: 99.66%

Biological Description

Chemical Properties

Storage & Solubility Information

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&IC50	PDE4B: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 x 105-fold versus PDE1, PDE2, PDE3, PDE5, and PDE6 and >2.5 x 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]

Molecular Weight	518.58
Formula	C27H26N4O5S
CAS No.	801312-28-7

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 10 mg/mL (19.28 mM)

References and Literature

1. Tralau-Stewart CJ, et al. J Pharmacol Exp Ther, 2011, 337(1), 145-154. 2. Woodrow MD, et al. Bioorg Med Chem Lett, 2009, 19(17), 5261-5265. 3. Nials AT, et al. J Pharmacol Exp Ther, 2011, 337(1), 137-144.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Neurodegenerative Disease Compound Library Drug Repurposing Compound Library Inhibitor Library Bioactive Compound Library ReFRAME Related Library Clinical Compound Library Anti-Alzheimer's Disease Compound Library NO PAINS Compound Library Bioactive Compounds Library Max Anti-Metabolism Disease Compound Library

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Keywords

GSK256066 801312-28-7 Metabolism PDE Phosphodiesterase (PDE) obstructive disease chronic high-affinity inhibit phosphodiesterase PDE4B Inhibitor GSK 256066 pulmonary GSK-256066 inhibitor

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