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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).
Sold for research purposes under agreement from GlaxoSmithKline
|Storage||Store at RT|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 500.57. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|0.5 mM||4 mL||19.98 mL||39.95 mL|
|2.5 mM||0.8 mL||4 mL||7.99 mL|
|5 mM||0.4 mL||2 mL||4 mL|
|25 mM||0.08 mL||0.4 mL||0.8 mL|
References are publications that support the biological activity of the product.
Johnson (1995) The anti-inflammatory profile of flutic. propionate. Allergy 50 11 PMID: 7604948
Zhang et al (2000) Enhancement of human eosinophil apoptosis by flutic. propionate, budesonide, and beclometh. Eur.J.Pharmacol. 406 325 PMID: 11040338
Smith and Kreutner (1998) In vitro glucocorticoid receptor binding and transcriptional activation by topically active glucocorticoids. Arzneim.-Forsch. 48 956
Pan et al (2012) Potentiation of the Kv1 family K+ channel by cortisone analogues. ACS Chem.Biol. 7 1641 PMID: 22803826
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Keywords: Fluticasone propionate, Fluticasone propionate supplier, Selective, high, affinity, glucocorticoid, agonists, Receptors, GlaxoSmithKline, GSK, Glucocorticoid, Receptor, Voltage-Gated, Potassium, Channels, 2007, Tocris Bioscience
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Literature in this Area
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Major depressive disorder is characterized by depressed mood and a loss of interest and/or pleasure. Updated in 2015 this poster highlights presynaptic and postsynaptic targets for the potential treatment of major depressive disorder, as well as outlining the pharmacology of currently approved antidepressant drugs.