• 产品描述： 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

• 靶点： hSGLT2:7.38 nM (IC50);hSGLT1:1876 nM (IC50);rSGLT2:6.73 nM (IC50);rSGLT1:1166 nM (IC50);mSGLT2:5.64 nM (IC50);mSGLT1:1380 nM (IC50)

• 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。 Cell Viability Assay Cell Line: MCF-7 human breast cancer cell lines Concentration: 1, 10, 50 μM Incubation Time: 24, 48, 72, 96 hours Result: Decreased the number of MCF-7 cells in a dose-dependent manner.

• 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 Administration Streptozotocin (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.

• 参考文献：
  1. Atsuo Tahara, et al. Pharmacological profile of ipragliflozin (ASP1941), a novel selective SGLT2 inhibitor, in vitro and in vivo. Naunyn Schmiedebergs Arch Pharmacol. 2012 Apr;385(4):423-36. 2. Shiho Komatsu, et al. SGLT2 inhibitor ipragliflozin attenuates breast cancer cell proliferation. Endocr J. 2020 Jan 28;67(1):99-106.

• 溶解性： Soluble  in  DMSO、H2O

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	2.472 ml	12.362 ml	24.725 ml
  5 mM	0.494 ml	2.472 ml	4.945 ml
  10 mM	0.247 ml	1.236 ml	2.472 ml
  50 mM	0.049 ml	0.247 ml	0.494 ml

• 注意：部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *