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Submit ReviewFluticasone propionate is a 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
Fluticasone propionate is also offered as part of the Tocriscreen FDA-Approved Drugs. 了解 Tocris 化合物库的更多信息。
分子量 | 500.57 |
公式 | C25H31F3O5S |
储存 | Store at RT |
纯度 | ≥98% (HPLC) |
CAS Number | 80474-14-2 |
PubChem ID | 444036 |
InChI Key | WMWTYOKRWGGJOA-CENSZEJFSA-N |
Smiles | O=C1C=C[C@@]2(C)C([C@@H](F)C[C@]3([H])[C@@](F)2[C@@H](O)C[C@@]4(C)[C@]([H])3C[C@@H](C)[C@](C(SCF)=O)4OC(CC)=O)=C1 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 25.03 | 50 |
以下数据基于产品分子量 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.
浓度/溶剂体积/质量 | 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 |
参考文献是支持产品生物活性的出版物。
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
If you know of a relevant reference for Fluticasone propionate, please let us know.
关键词: 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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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.