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Beschreibung

A cell permeable, spirocyclic urea that acts as a selective inhibitor of 11beta-hydroxysteroid dehydrogenase 1 (11beta-HSD1) (IC50 of 1.6 nM and 5.3 nM) in enzyme and human adipocyte assays, respectively. Consisting of 2 enantiomers, 10j2 (R Isomer) is shown to be ˜, 2-3X more potent than 10j1 (S Isomer), in both aforementioned assays. 11beta-HSD1 activity in the presence of 10j2 (10mg/kg in animals p.o.) results in an ˜, 80% reduction in the concentration of plasma cortisol over vehicle treated controls., A cell permeable, spirocyclic urea that acts as a selective inhibitor of 11beta-hydroxysteroid dehydrogenase 1 (11beta-HSD1) (IC50 of 1.6 nM and 5.3 nM) in enzyme and human adipocyte assays, respectively. Consisting of 2 enantiomers, 10j2 (R Isomer) is shown to be ˜, 2-3X more potent than 10j1 (S Isomer), in both aforementioned assays. 11beta-HSD1 activity in the presence of 10j2 (10 mg/kg in animals p.o.) results in an ~80% reduction in the concentration of plasma cortisol over vehicle treated controls.