GW 870086

GW 870086 is a cyano- and isopropyl-substituted derivative of the synthetic corticosteroid and glucocorticoid receptor agonist fluticasone propionate (Item No. 20703).¹ It selectively inhibits TNF-α-induced transcriptional activity of NF-κB 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-α-induced increases in the expression of mRNA encoding COX-2 and TNF-C, also known as lymphotoxin-β (LT-β), in A549 lung cancer cells. It inhibits TNF-α-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.

WARNING This product is not for human or veterinary use.

1. Uings, I.J., Needham, D., Matthews, J., et al. Discovery of GW870086: A potent anti-inflammatory steroid with a unique pharmacological profile. Br. J. Pharmacol. 169(6), 1389-1403 (2013).