Fluticasone propionate

Biological Activity

Fluticasone propionate is a high affinity, selective glucocorticoid receptor agonist (K_d = 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 K_V1 channels (EC₅₀ = 37 nM).

Technical Data

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Additional Information

Background References

1. Regulation of the CCL2 Gene in Pancreatic beta-Cells by IL-1beta and Glucocorticoids: Role of MKP-1.
   Burke S, Goff M, Updegraff B, Lu D, Brown P, Minkin S, Biggerstaff J, Zhao L, Karlstad M, Collier J
   PLoS ONE, 2012;7(10):e46986.
2. Potentiation of the Kv1 family K⁺ channel by cortisone analogues.
   Pan et al.
   ACS Chem.Biol., 2012;7:1641
3. In vitro glucocorticoid receptor binding and transcriptional activation by topically active glucocorticoids.
   Smith and Kreutner
   Arzneim.-Forsch., 1998;48:956
4. The anti-inflammatory profile of flutic. propionate.
   Johnson
   Allergy, 1995;50:11
5. Enhancement of human eosinophil apoptosis by flutic. propionate, budesonide, and beclometh.
   Zhang et al.
   Eur.J.Pharmacol., 2000;406:325

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