(R)-BMS-816336 NLT 98%

(R)-BMS-816336 (Compound 6n-1) is a potent and orally active inhibitor of human, mouse and cynomolgus monkey 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) enzyme with IC₅₀s of 14.5 nM, 50.3 nM and 16 nM, respectively ^[1]. IC50 & Target: IC50: 14.5 nM (Human 11β-HSD1), 50.3 nM (Mouse 11β-HSD1) and 16 nM (Cynomolgus monkey 11β-HSD1)^[1] In Vivo: During the in vivo studies of BMS-816336 (Compound 6n-2) in animals, its enantiomer (R)-BMS-816336 (Compound 6n-1) in the plasma samples, together with trace amount of Ketone A are detected. The interconversion of BMS-816336 and (R)-BMS-816336 take place via the intermediate Ketone A through physiological oxidation and reduction process. In vivo studies in rat, dog, and cynomolgus monkey, the plasma ratios of (R)-BMS-816336/BMS-816336 decrease in the order: dog ≫ rat >cynomolgus monkey^[1].