1346554-47-9
1346554-47-9 結(jié)構(gòu)式
基本信息
中文別名
化合物 T28796 英文別名
SKI-28524-Pyrimidinecarboxamide, 2-[(2R)-4-[2-fluoro-4-(methylsulfonyl)phenyl]-2-methyl-1-piperazinyl]-N-[5-hydroxytricyclo[3.3.1.13,7]dec-2-yl]-
物理化學(xué)性質(zhì)
密度1.44±0.1 g/cm3(Predicted)
酸度系數(shù)(pKa)12.28±0.40(Predicted)
形態(tài)Solid
顏色White to off-white
應(yīng)用領(lǐng)域
用途一
SKI2852 is a Highly Potent, Selective, and Orally Bioavailable Inhibitor of 11β-Hydroxysteroid Dehydrogenase Type 1 (11β-HSD1) potentially for treatment of diabetics. SKI2852 bioactivity data: hHSD1 IC50 = 2.9nM; mHSD1 IC50 = 1.6nM; HEK293 IC50 = 4/4 nM; Mous PK: 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 oral administration of SKI2852 significantly reduced blood glucose and HbA1c levels and improved the lipid profiles in ob/ob mice.