Pricing updated 2019-03-24. Prices are subject to change without notice.
AL 082D06 is a non-steroidal antagonist of the glucocorticoid receptor (GR; Ki = 210 nM; EC50 = 0.3 nM in a luciferase assay).1 It is selective for GR over the androgen, progesterone, mineralocorticoid, and estrogen receptors with Ki values greater than 4, 3, 3, and 10 µM, respectively. AL 082D06 inhibits transcriptional activation induced by glucocorticoids and reverses dexamethasone-mediated repression of gene expression in a luciferase reporter assay. It blocks GR binding to DNA in vitro when induced by either dexamethasone (Item No. 11015) or mifepristone (Item No. 10006317). In contrast to the steroid-type GR antagonists ZK-299 and mifepristone, GR bound to AL 082D06 does not compete with a constitutively active GR.
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1. Miner, J.N., Tyree, C., Hu, J., et al. A nonsteroidal glucocorticoid receptor antagonist Mol. Endocrinol. 17(1), 117-127 (2003).