Fluticasone Propionate

Fluticasone propionate is a synthetic corticosteroid and glucocorticoid receptor agonist. It inhibits AP-1-mediated transcription in a transrepression assay using ChaGo-K-1 cells (IC50 = 0.04 nM). 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 alpha (ERalpha) and ERbeta (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). 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. 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). Formulations containing fluticasone propionate have been used in the treatment of allergic and non-allergic rhinitis.Formal Name: (6alpha,11beta,16alpha,17alpha)-6,9-difluoro-11-hydroxy-16-methyl-3-oxo-17-(1-oxopropoxy)androsta-1,4-diene-17-carbothioic acid, S-(fluoromethyl) ester. CAS Number: 80474-14-2. Synonyms: Fluticasone 17-Propionate. Molecular Formula: C25H31F3O5S. Formula Weight: 500.6. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 25 mg/ml, DMSO: 25 mg/ml, DMSO:PBS (pH 7.2) (1:3): 0.25 mg/ml, Ethanol: 1 mg/ml. lambdamax: 235 nm. SMILES: O=C1C=C[C@@]2(C)C([C@@H](F)C[C@]3([H])[C@]2(F)[C@@H](O)C[C@@]4(C)[C@@]3([H])C[C@@H](C)C4(OC(CC)=O)C(SCF)=O)=C1. InChi Code: InChI=1S/C25H31F3O5S/c1-5-20(31)33-25(21(32)34-12-26)13(2)8-15-16-10-18(27)17-9-14(29)6-7-22(17,3)24(16,28)19(30)11-23(15,25)4/h6-7,9,13,15-16,18-19,30H,5,8,10-12H2,1-4H3/t13-,15+,16+,18+,19+,22+,23+,24+,25?/m1/s1. InChi Key: WMWTYOKRWGGJOA-JUHDKXAESA-N.