BVT-2733 is an inhibitor of 11β-hydroxysteroid dehydrogenase 1 (11β-HSD1) that exhibits anti-diabetic, anti-inflammatory, and anti-osteoporotic properties. BVT-2733 decreases blood glucose and serum insulin levels in animal models of hyperglycemia. BVT-2733 also attenuates arthritis severity, decreases pro-inflammatory cytokine production, and suppresses synovial inflammation. In other animal models, this compound prevents 11βHSD-induced osteogenic differentiation and suppression of osteogenesis. BVT-2733 had reasonable mouse potency (IC50 = 96nM) but was only weakly active against the human isoform (IC50 = 3341 nM). This combined with moderate mouse pharmacokinetics (F = 21%) made it a suitable in vivo tool with which to explore the potential of 11β-HSD1 as a mechanism for the treatment of type II diabetes. In KKAy mice, oral dosing twice daily (25, 50, 100 mg/kg) of BVT-2733 lowered blood glucose levels in a dose-dependent manner.