| Identification | Back Directory | [Name]
GSK-256066 (2,2,2-trifluoroacetic acid) | [CAS]
1415560-64-3 | [Synonyms]
GSK256066 (2
GSK-256066; GSK 256066
2-trifluoroacetic acid)
GSK256066 trifluoroacetate
GSK-256066 (2,2,2-trifluoroacetic acid)
GSK256066 Trifluoroacetate,GSK-256066 Trifluoroacetate
6-[[3-[(Dimethylamino)carbonyl]phenyl]sulfonyl]-4-[(3-methoxyphenyl)amino]-8-methyl-3-quinolinecarboxamide 2,2,2-trifluoroacetate (1:1) | [Molecular Formula]
C29H27F3N4O7S | [MDL Number]
MFCD22125307 | [MOL File]
1415560-64-3.mol | [Molecular Weight]
632.61 |
| Hazard Information | Back Directory | [Uses]
GSK256066 Trifluoroacetate is a selective and high-affinity phosphodiesterase 4 (PDE) inhibitor, with an IC50 of 3.2 pM for PDE4B. GSK256066 Trifluoroacetate is developed for the research of chronic obstructive pulmonary disease[1]. | [in vivo]
GSK256066 Trifluoroacetate (0.3-100 μg/kg; intratracheally) inhibits the eosinophil number increased in the bronchoalveolar lavage (BAL) in a dose-dependent fashion, in lipopolysaccharide (LPS)- and ovalbumin (OVA)-induced acute pulmonary inflammation rat models.[2].
GSK256066 Trifluoroacetate inhibits LPS-induced pulmonary neutrophilia, and no emetic episodes are observed in ferrets[2].
| Animal Model: | Male Brown Norway rats(180-200 g)[2] | | Dosage: | 0.3-100 μg/kg | | Administration: | Intratracheally; 30 minutes before and 6 hours after ovalbumin challenge | | Result: | Inhibited the increase in eosinophil number in the BAL in a dose-dependent fashion. |
| [storage]
Store at -20°C | [References]
[1] Tralau-Stewart CJ, et al. GSK256066, an exceptionally high-affinity and selective inhibitor of phosphodiesterase 4 suitable for administration by inhalation: in vitro, kinetic, and in vivo characterization. J Pharmacol Exp Ther, 2011, 337(1), 145-154. DOI:10.1124/jpet.110.173690
[2] Nials AT, et al. In vivo characterization of GSK256066, a high-affinity inhaled phosphodiesterase 4 inhibitor. J Pharmacol Exp Ther, 2011, 337(1), 137-144. DOI:10.1124/jpet.110.173641 |
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| Company Name: |
SPIRO PHARMA
|
| Tel: |
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| Website: |
www.spiropharma.com.cn |
| Company Name: |
BOC Sciences
|
| Tel: |
16314854226 |
| Website: |
www.bocsci.com |
| Company Name: |
Musechem
|
| Tel: |
+1-800-259-7612 |
| Website: |
www.musechem.com |
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