GW 870086

GW 870086 is a cyano- and isopropyl-substituted derivative of the synthetic corticosteroid and glucocorticoid receptor agonist fluticasone propionate (Cay-20703). It selectively inhibits TNF-alpha-induced transcriptional activity of NF-kappaB in a reporter assay using A549 cells (IC50 = 0.08 nM) over a panel of 50 steroid receptors in reporter assays using CV-1 cells at 1 µM. GW 870086 (5 nM) prevents TNF-alpha-induced increases in the expression of mRNA encoding COX-2 and TNF-C, also known as lymphotoxin-beta (LT-beta), in A549 lung cancer cells. It inhibits TNF-alpha-induced increases in IL-8 secretion in 16HBE bronchial epithelial cells in a concentration-dependent manner. In vivo, GW 870086 (30 µg/animal) reduces oxazolone-induced increases in ear swelling in a mouse model of contact dermatitis, as well as inhibits ovalbumin-induced bronchoconstriction and increases in the number of eosinophils in the bronchoalveolar lavage fluid (BALF) in mice when administered at doses of 30 or 100 µg/animal per day.Formal Name: 6alpha,9-difluoro-11beta-hydroxy-16alpha-methyl-3-oxo-17alpha-[[(2,2,3,3-tetramethylcyclopropyl)carbonyl]oxy]-androsta-1,4-diene-17-carboxylic acid, cyanomethyl ester. CAS Number: 827319-43-7. Molecular Formula: C31H39F2NO6. Formula Weight: 559.6. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMSO: Soluble: >10 mg/ml, Ethanol: Slightly soluble: 0.1-1 mg/ml, Methanol: Slightly soluble: 0.1-1 mg/ml. SMILES: C[C@@]12[C@@](OC(C3C(C)(C)C3(C)C)=O)(C(OCC#N)=O)[C@H](C)C[C@@]1([H])[C@@]4([H])[C@]([C@H](C2)O)([C@@]5(C([C@H](C4)F)=CC(C=C5)=O)C)F. InChi Code: InChI=1S/C31H39F2NO6/c1-16-12-18-19-14-21(32)20-13-17(35)8-9-28(20,6)30(19,33)22(36)15-29(18,7)31(16,25(38)39-11-10-34)40-24(37)23-26(2,3)27(23,4)5/h8-9,13,16,18-19,21-23,36H,11-12,14-15H2,1-7H3/t16-,18+,19+,21+,22+,28+,29+,30+,31+/m1/s1. InChi Key: WUBKGTSFJSEIEM-NSHBDUGJSA-N.