Catalog Number: 2007
Chemical Name: (6α,11β,16α,17α)-6,9-Difluoro-11-hydroxy-16-methyl-3-oxo-17-(1-oxopropoxy)androsta-1,4-diene-17-carbothioic acid fluoromethyl ester
Biological Activity
High affinity, selective glucocorticoid receptor agonist (Kd = 0.5 nM). Potently stimulates glucocorticoid receptor-mediated transactivation of gene expression and enhances human eosinophil apoptosis (EC50 = 3.7 nM) in vitro. Inhibits mast cell accumulation in nasal mucosa following topical administration. Lipophilic anti-inflammatory agent with low oral bioavailability. Also potentiates KV1 channels (EC50 = 37 nM).
Technical Data
  • M.Wt:
    500.57
  • Formula:
    C25H31F3O5S
  • Solubility:
    Soluble to 50 mM in DMSO
  • Purity:
    >98%
  • Storage:
    Store at RT
  • CAS No:
    80474-14-2
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Additional Information
Licensing Caveats:
Sold for research purposes under agreement from GlaxoSmithKline
Background References
  1. The anti-inflammatory profile of fluticasone propionate.
    Johnson
    Allergy, 1995;50:11
  2. Enhancement of human eosinophil apoptosis by fluticasone propionate, budesonide, and beclomethasone.
    Zhang et al.
    Eur.J.Pharmacol., 2000;406:325
  3. Potentiation of the Kv1 family K+ channel by cortisone analogues.
    Pan et al.
    ACS Chem.Biol., 2012;7:1641
  4. In vitro glucocorticoid receptor binding and transcriptional activation by topically active glucocorticoids.
    Smith and Kreutner
    Arzneim.-Forsch., 1998;48:956

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