产品
编 号:F451778
分子式:C21H21FO5S
分子量:404.45
产品类型
结构图
CAS No: 761423-87-4
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生物活性:
Ipragliflozin (ASP1941) is an orally active and selective SGLT2 inhibitor with IC50s of 7.38 and 1876 nM, 6.73 and 1166 nM, 5.64 and 1380 nM for human SGLT2 and SGLT1, rat SGLT2 and SGLT1, mouse SGLT2 and SGLT1, respectively. Antidiabetic agent.
体内研究:
Ipragliflozin 具有抗高血糖作用。Ipragliflozin (0.1-1 mg/kg) 剂量依赖性地抑制血糖水平的升高。在 STZ 诱导的 1 型糖尿病大鼠中,该效应在 0.3 和 1 mg/kg 剂量下显著,而在 KK-Ay 2 型糖尿病小鼠中,该效应在所有测试剂量下均显著。 Ipragliflozin (0.3 和 1 mg/kg) 在链脲佐菌素诱导的 1 型糖尿病大鼠中显示出重复给药的抗糖尿病作用。Animal Model:Single AdministrationStreptozotocin (STZ; 50 mg/kg)-induced type 1 diabetic rats and KK-Ay type 2 diabetic mice
Dosage:0.1-1 mg/kg
Administration:Single oral administration in the fed condition. Blood glucose levels were then measured for 8 h under fasting conditions.
Result:Dose-dependently lowered blood glucose levels, and this effect was significant at all tested doses.
Animal Model:Repeated AdministrationStreptozotocin (STZ; 50 mg/kg)-induced type 1 diabetic rats
Dosage:0.3 and 1 mg/kg
Administration:Administration orally once daily (at night) for 4 weeks.
Result:Significantly reduced the levels of HbA1c and blood glucose. Pancreatic insulin content was significantly increased at a dose of 1 mg/kg. Urinary glucose excretion was increased dose-dependently, and this was significant at the 1 mg/kg dose.
体外研究:
Ipragliflozin (1-50 μM) 显著且剂量依赖性地抑制 MCF-7 人乳腺癌细胞系的生长。 在使用siRNA 敲低SGLT2 表达后,Ipragliflozin 诱导的细胞增殖减弱被完全取消,表明Ipragliflozin 通过抑制SGLT2 减弱乳腺癌细胞增殖。 BrdU 测定显示高剂量 (50 和 100 μM) Ipragliflozin 显著抑制 MCF-7 细胞的 DNA 合成。