SKI-2852

A highly potent, selective, and orally bioavailable 11β-HSD1 inhibitor with IC50 of 2.9 and 1.6 nM for hHSD1 and mHSD1, respectively; demonstrates no CYP and PXR liabilities, excellent PK profiles across species, and highly potent and sustainable PD activity; significantly reduces blood glucose and HbA1c levels and improves the lipid profiles in ob/ob mice, synergistically enhances the HbA1c-lowering effect of metformin in vivo.

References 1. Ryu JH, et al. J Med Chem. 2016 Nov 23;59(22):10176-10189. View Related Products by Target 11β-HSD