HSD-016

HSD-016 is a potent, selective, and orally active small molecule inhibitor of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1). This enzyme catalyzes the conversion of inactive cortisone to active cortisol. By inhibiting 11β-HSD1, HSD-016 aims to reduce local tissue glucocorticoid activation and has been investigated as a therapeutic candidate for diabetes and metabolic syndrome. The compound demonstrated strong inhibitory effects on human (IC50 = 11 nM), mouse (IC50 = 1 nM), and rat (IC50 = 8 nM) forms of the enzyme. It was advanced into phase I clinical trials but no further development status is currently available[2][3][5][6].

Other names

(R)-1,1,1-trifluoro-2-(3-((R)-4-(4-fluoro-2-(trifluoromethyl)phenyl)-2-methylpiperazin-1-ylsulfonyl)phenyl)propan-2-ol