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GSK 256066 Trifluoroacetate

CAS No. 1415560-64-3

GSK 256066 Trifluoroacetate ( GSK-256066;GSK256066 (2,2,2-trifluoroacetic acid) )

Catalog No. M11725 CAS No. 1415560-64-3

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

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    GSK 256066 Trifluoroacetate
  • Note
    Research use only, not for human use.
  • Brief Description
    A potent, selective PDE4 inhibitor with pIC50 of 11.5, 11.3, 11.4, and 11.9 for PDE4B, A, C, and D, respectively.
  • Description
    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
  • Synonyms
    GSK-256066;GSK256066 (2,2,2-trifluoroacetic acid)
  • Pathway
    Angiogenesis
  • Target
    PDE
  • Recptor
    PDE
  • Research Area
    Inflammation/Immunology
  • Indication
    COPD

Chemical Information

  • CAS Number
    1415560-64-3
  • Formula Weight
    632.61
  • Molecular Formula
    C29H27F3N4O7S
  • Purity
    >98% (HPLC)
  • Solubility
    10 mM in DMSO
  • SMILES
    CC1=CC(=CC2=C(C(=CN=C12)C(=O)N)NC3=CC(=CC=C3)OC)S(=O)(=O)C4=CC=CC(=C4)C(=O)N(C)C.C(=O)(C(F)(F)F)O
  • Chemical Name
    3-Quinolinecarboxamide, 6-[[3-[(dimethylamino)carbonyl]phenyl]sulfonyl]-4-[(3-methoxyphenyl)amino]-8-methyl-, 2,2,2-trifluoroacetate (1:1)

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

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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