Tofogliflozin (hydrate)

SGLT2的强效抑制剂（人、大鼠和小鼠SGLT2的Kis分别为2.9、14.9和6.4nM）；对SGLT2具有选择性（IC50=2.9nM），优于其他SGLT（SGLT1和3-6的IC50=>1,500nM）；在剂量范围为3-10mg/kg的条件下，可降低Zucker糖尿病肥胖大鼠的血浆葡萄糖浓度并以剂量依赖性方式增加肾脏葡萄糖清除率；可降低非禁食db/db小鼠的高血糖症，并降低GK大鼠（一种伴有葡萄糖不耐受的2型糖尿病非肥胖模型）的餐后高血糖症。A potent inhibitor of SGLT2 (Kis = 2.9, 14.9, and 6.4 nM for human, rat, and mouse SGLT2, respectively); selective for SGLT2 (IC50 = 2.9 nM) over other SGLTs (IC50s = >1,500 nM for SGLT1 and 3-6); reduces plasma glucose concentration and increases renal glucose clearance in Zucker diabetic fatty rats in a dose-dependent manner when administered at doses ranging from 3-10 mg/kg; reduces hyperglycemia in non-fasted db/db mice and decreases postprandial hyperglycemia in GK rats, a non-obese model of type 2 diabetes with glucose intolerance.