AZD8329 is a potent 11β-Hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor with an IC50 of 9 nM for human 11β-HSD1, displays excellent selectivity versus 11β-HSD2, 17β-HSD1 and 17β-HSD3[1]. IC50: 9 nM (Human 11β-HSD1)[1]
AZD8329 shows IC50s of 0.009, 0.0086, 0.008, 0.024, 0.002 and 6.1 μM for human enzyme, rat enzyme, dog enzyme, cyno enzyme, human adipocyte and mouse enzyme, respectively[1].
[1]. Scott JS, et al. Novel acidic 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor with reduced acyl glucuronide liability: the discovery of 4-[4-(2-adamantylcarbamoyl)-5-tert-butyl-pyrazol-1-yl]benzoic acid (AZD8329). J Med Chem. 2012 Nov 26;55(22):10136-47.