Fluticasone Furoate

Fluticasone furoate is a synthetic glucocorticoid. It is selective for the glucocorticoid receptor over the mineralocorticoid, progesterone, and androgen receptors in reporter assays (EC50s = 0.03, 23.4, 0.9, and >10,000 nM, respectively), as well as estrogen receptor alpha (ERalpha) and ERbeta in scintillation proximity assays (EC50s = >10,000 nM for both). Fluticasone furoate reduces LPS-induced increases in TNF-alpha production in human peripheral blood mononuclear cells (PBMCs) with an EC50 value of 0.12 nM. It decreases S. aureus enterotoxin-induced increases in IFN-gamma, IL-2, IL-5, IL-17, and TNF-alpha levels in patient-derived nasal polyp tissue when used at a concentration of 100 nM. Intrathecal administration of fluticasone furoate (30 µg/animal) reduces ovalbumin-induced increases in bronchoalveolar lavage fluid (BALF) eosinophil infiltration in a rat model of allergic inflammation. Formulations containing fluticasone furoate have been used in the treatment of seasonal allergies.Formal Name: (6alpha,11beta,16alpha,17alpha)-6,9-difluoro-17-[(2-furanylcarbonyl)oxy]-11-hydroxy-16-methyl-3-oxo-androsta-1,4-diene-17-carbothioic acid, S-(fluoromethyl) ester. CAS Number: 397864-44-7. Synonyms: GSK685698, GW 685698X. Molecular Formula: C27H29F3O6S. Formula Weight: 538.6. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMF: 20 mg/ml, DMF:PBS (pH 7.2) (1:3): 0.25 mg/ml, DMSO: 15 mg/ml, Ethanol: 1 mg/ml. lambdamax: 242 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)[C@]4(OC(C5=CC=CO5)=O)C(SCF)=O)=C1. InChi Code: InChI=1S/C27H29F3O6S/c1-14-9-16-17-11-19(29)18-10-15(31)6-7-24(18,2)26(17,30)21(32)12-25(16,3)27(14,23(34)37-13-28)36-22(33)20-5-4-8-35-20/h4-8,10,14,16-17,19,21,32H,9,11-13H2,1-3H3/t14-,16+,17+,19+,21+,24+,25+,26+,27+/m1/s1. InChi Key: XTULMSXFIHGYFS-VLSRWLAYSA-N.