Research Area
Product Type
United States ( Change Country )
GSK256066 Chemical Structure
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Biological Activity
GSK256066 is an exceptionally high affinity and selective PDE4 inhibitor with an IC50 of 3.2 pM for PDE4B. GSK256066 suppressed tumor necrosis factor α production by lipopolysaccharide (LPS)-stimulated human peripheral blood monocytes with 0.01 nM IC50 (compared with IC50 values of 5, 22, and 389 nM for roflumilast, tofimilast, and cilomilast, respectively) and by LPS-stimulated whole blood with 126 pM IC50. GSK256066 also inhibited LPS-induced increases in exhaled nitric oxide (ED50=35 µg/kg). In addition, GSK256066 prevented pulmonary eosinophilia in rats exposed to ovalbumin (ED50=0.4 μg/kg). In ferrets, inhaled GSK256066 inhibited LPS-induced pulmonary neutrophilia (ED50=18 μg/kg) and no emetic episodes were observed. [1][2]
References on GSK256066
- [1] J Pharmacol Exp Ther. 2011 Apr;337(1):137-44.
- [2] Respir Res. 2010 Mar 1;11:26.
Chemical Information
| Molecular Weight (WM): | 518.58 |
|---|---|
| Formula: | C27H26N4O5S |
| CAS No.: | 801312-28-7 |
| Synonyms: |
N/A
|
| Dissolve in (25°C): | DMSO ≥5mg/mL |
| Water <1mg/mL | |
| Ethanol <1mg/mL | |
| Storage: | 2 years-20°CPowder |
| 1 week-4°Cin DMSO | |
| 1 month-80°in DMSO |
Quality Control & MSDS
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