Chemical Name |
GSK 256066 Trifluoroacetate |
CAS Number |
1415560-64-3 |
MDL Number |
MFCD22125307 |
Molecular Formula |
C29H27F3N4O7S |
Molecular Weight |
632.61 |
Synonyms |
GSK256066 (2,2,2-trifluoroacetic acid) |
Introduction of 1415560-64-3 :
GSK 256066 Trifluoroacetate (GSK256066 2,2,2-trifluoroacetic acid) is a selective and high-affinity phosphodiesterase 4 (PDE) inhibitor, with an IC50 of 3.2 pM for PDE4B; developed for the treatment of chronic obstructive pulmonary disease[1]. IC50 & Target: IC50: 3.2 pM (PDE4B)[1] In Vitro: GSK 256066 Trifluoroacetate (GSK256066 2,2,2-trifluoroacetic acid) is an exceptionally high-affinity inhibitor of PDE4 designed for inhaled administration[1].
GSK 256066 Trifluoroacetate is highly selective for PDE4, with >380,000-fold versus PDE1/2/3/5/6 and >2500-fold against PDE7, and inhibits PDE4 isoforms A-D with equal affinity[1].
GSK 256066 Trifluoroacetate inhibits tumor necrosis factor α production by lipopolysaccharide (LPS)-stimulated human peripheral blood monocytes with IC50 of 0.01 nM[1].
In Vivo: GSK 256066 Trifluoroacetate (GSK256066 2,2,2-trifluoroacetic acid; 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].
GSK 256066 Trifluoroacetate inhibits LPS-induced pulmonary neutrophilia, and no emetic episodes are observed in ferrets[2].
Purity |
NLT 98% |
Storage |
at 20ºC 2 years |
*The above information is for reference only.