Figure 1From: A novel 11β-hydroxysteroid dehydrogenase type1 inhibitor CNX-010-49 improves hyperglycemia, lipid profile and reduces body weight in diet induced obese C57B6/J mice with a potential to provide cardio protective benefits Potency and selectivity of CNX-010-49. Inhibition curve with increasing concentrations of CNX-010-49 for reductase activity in CHOK1 cells stably expressing human 11β-HSD1 (A), Mouse C2C12 cells (B), fully differentiated human adipocytes (C), both reductase and dehydrogenase activity with recombinant human 11β-HSD1 protein (D) as mentioned in the materials and methods. Selectivity of CNX-010-49 (100 μM) against HSD related enzymes were evaluated in CHOK1 cells transiently over expressing human 11βHSD2 and 17β HSD3 respectively (E & G) and T47D cells for 17βHSD1 (F). Data are means of three individual experiments with standard deviations (n = 6).Back to article page