SKI2852 is a Highly Potent, Selective, and orally Bioavailable Inhibitor of 11β-Hydroxysteroid Dehydrogenase Type 1 (11β-HSD1) potentially for treatment of diabetics. SKI2852 hHSD1 IC50 = 2.9nM; mHSD1 IC50 = 1.6nM; HEK293 IC50 = 4/4 nM; F = 96%; CYP3A4 IC50 > 10 μM; CYP2C19 IC50 > 10 μM. SKI2852 demonstrated no CYP and PXR liabilities, excellent PK profiles across species, and highly potent and sustainable PD activity. Repeated orally bioavailable administration of SKI2852 significantly reduced blood glucose and HbA1c levels and improved the lipid profiles in ob/ob mice. References: Ryu JH, Lee JA, Kim S, Shin YA, Yang J, Han HY, Son HJ, Kim YH, Sa JH, Kim JS, Lee J, Lee J, Park HG. Discovery of 2-((R)-4-(2-Fluoro-4-(methylsulfonyl)phenyl)-2-methylpiperazin-1-yl)-N-((1R,2s,3S ,5S,7S)-5-hydroxyadamantan-2-yl)pyrimidine-4-carboxamide (SKI2852): A Highly Potent, Selective, and Orally Bioavailable Inhibitor of 11β-Hydroxysteroid Dehydrogenase Type 1 (11β-HSD1). J Med Chem. 2016 Oct 31. [Epub ahead of print] PubMed PMID: 27798827.

纯度：≥98%

CAS：1346554-47-9