Fluticasone Propionate

Territorial Availability: Available through Bertin Technologies only in France

• Synonyms
  • (6?,11?,16?,17?)-6,9-difluoro-11-hydroxy-16-methyl-3-oxo-17-(1-oxopropoxy)androsta-1,4-diene-17-carbothioic acid, S-(fluoromethyl) ester
• Correlated keywords
  • rhinitis COPD intranasal corticosteroid glucocorticoid anti-inflammatory lipophilic bio-available KV1 KV-1 flumethasone atemur mite axotide CCI18781 CCI-18781 cutivate cyclesonide flixonase flixotide flonase flovent flunase fluticone flutide flutivate rotadisk zoflut
• Product Overview:
  Fluticasone propionate is a synthetic corticosteroid and glucocorticoid receptor agonist.{69133} It inhibits AP-1-mediated transcription in a transrepression assay using ChaGo-K-1 cells (IC50 = 0.04 nM).{69133} Fluticasone propionate selectively binds to the glucocorticoid receptor (IC50 = 0.0009 µM) over the progesterone, mineralocorticoid, and androgen receptors (IC50s = 0.021, 0.149, and >10 µM, respectively), as well as estrogen receptor ? (ER?) and ER? (IC50s = >10 µM for both). It increases apoptosis of T cells isolated from human peripheral blood in a concentration-dependent manner and induces spontaneous apoptosis of primary human eosinophils (EC50 = 3.7 nM).{46116,69135} Fluticasone propionate completely inhibits congestion in a guinea pig model of allergic rhinitis induced by ovalbumin when administered as a 0.5 mg/ml solution at 20 µl/nostril.{64191} It reduces ovalbumin-induced increases in IL-4 in nasal lavage fluid in the same model. Fluticasone propionate also potentiates voltage-dependent potassium channel 1 (Kv1) currents in an inside-out patch-clamp assay (EC50 = 37 nM).{69134} Formulations containing fluticasone propionate have been used in the treatment of allergic and non-allergic rhinitis.