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GSK-256066

Chemical Structure : GSK-256066

CAS No.: 801312-28-7

GSK-256066 (GSK256066;GSK 256066)

Catalog No.: PC-42606Not For Human Use, Lab Use Only.

A potent, selective PDE4 inhibitor with pIC50 of 11.5, 11.3, 11.4, and 11.9 for PDE4B, A, C, and D, respectively.

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10 mg $220 In stock
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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

A potent, selective PDE4 inhibitor with pIC50 of 11.5, 11.3, 11.4, and 11.9 for PDE4B, A, C, and D, respectively; displays >380,000-fold selectivity over PDE1/2/3/5/6/7; inhibits TNFα production by lLPS-stimulated human peripheral blood monocytes with IC50 of 0.01 nM; inhibites LPS-induced pulmonary neutrophilia with ED50 of 1.1 ug/kg (aqueous suspension) and 2.9 ug/kg (dry powder formulation) in rats.

COPD

Phase 2 Discontinued

Physicochemical Properties

M.Wt 518.5842
Formula C27H26N4O5S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMSO: ≥ 5.2 mg/mL

Chemical Name/SMILES

3-Quinolinecarboxamide, 6-[[3-[(dimethylamino)carbonyl]phenyl]sulfonyl]-4-[(3-methoxyphenyl)amino]-8-methyl-

References

1. Woodrow MD, et al. Bioorg Med Chem Lett. 2009 Sep 1;19(17):5261-5.

2. Tralau-Stewart CJ, et al. J Pharmacol Exp Ther. 2011 Apr;337(1):145-54.

3. Nials AT, et al. J Pharmacol Exp Ther. 2011 Apr;337(1):137-44.

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