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GSK-256066 2,2,2-trifluoroacetic acid

Chemical Structure : GSK-256066 2,2,2-trifluoroacetic acid

CAS No.: 1415560-64-3

GSK-256066 2,2,2-trifluoroacetic acid (GSK-256066)

Catalog No.: PC-45952Not 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 $200 In stock
50 mg $576 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 PDE1/23/5/6/7; 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 632.6075
Formula C29H27F3N4O7S
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

10 mM in DMSO

Chemical Name/SMILES

3-Quinolinecarboxamide, 6-[[3-[(dimethylamino)carbonyl]phenyl]sulfonyl]-4-[(3-methoxyphenyl)amino]-8-methyl-, 2,2,2-trifluoroacetate (1:1)

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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