Ipragliflozin

Ipragliflozin (ASP1941) is an orally active and selective inhibitor of SGLT2, with IC50s of 7.38 and 1876 nM for human SGLT2 and SGLT1, respectively. It serves as an antidiabetic agent¹.

In MCF-7 human breast cancer cell lines, Ipragliflozin (1-50 μM) significantly and dose-dependently suppresses growth. Knocking down SGLT2 expression using siRNA abolishes the attenuation of cell proliferation induced by Ipragliflozin, indicating its action through SGLT2 inhibition. Additionally, Ipragliflozin at high doses (50 and 100 μM) significantly inhibits DNA synthesis of MCF-7 cells, as revealed by BrdU assay².

Ipragliflozin exhibits antihyperglycemic effects, with dose-dependent inhibition of increases in blood glucose levels. In both STZ-induced type 1 diabetic rats and KK-Ay type 2 diabetic mice, this effect is significant at various tested doses¹.

In streptozotocin-induced type 1 diabetic rats, repeated administration of Ipragliflozin (0.3 and 1 mg/kg) demonstrates antidiabetic effects¹.

In Streptozotocin (STZ; 50 mg/kg)-induced type 1 diabetic rats and KK-Ay type 2 diabetic mice, doses ranging from 0.1 to 1 mg/kg were orally administered once in the fed state. Blood glucose levels were then monitored for 8 hours under fasting conditions. The results indicated a dose-dependent reduction in blood glucose levels, which was statistically significant at all tested doses. This experiment utilized a repeated administration animal model¹.

In Streptozotocin (STZ; 50 mg/kg)-induced type 1 diabetic rats, doses of 0.3 and 1 mg/kg were orally administered once daily at night for 4 weeks. The outcome revealed significant reductions in both HbA1c and blood glucose levels. Furthermore, pancreatic insulin content significantly increased at a dose of 1 mg/kg. Urinary glucose excretion exhibited a dose-dependent increase, reaching significance at the 1 mg/kg dose¹.

Ipragliflozin exhibits antihyperglycemic effects, with dose-dependent inhibition of increases in blood glucose levels. In both STZ-induced type 1 diabetic rats and KK-Ay type 2 diabetic mice, this effect is significant at various tested doses¹.

In streptozotocin-induced type 1 diabetic rats, repeated administration of Ipragliflozin (0.3 and 1 mg/kg) demonstrates antidiabetic effects¹.

In Streptozotocin (STZ; 50 mg/kg)-induced type 1 diabetic rats and KK-Ay type 2 diabetic mice, doses ranging from 0.1 to 1 mg/kg were orally administered once in the fed state. Blood glucose levels were then monitored for 8 hours under fasting conditions. The results indicated a dose-dependent reduction in blood glucose levels, which was statistically significant at all tested doses. This experiment utilized a repeated administration animal model¹.

In Streptozotocin (STZ; 50 mg/kg)-induced type 1 diabetic rats, doses of 0.3 and 1 mg/kg were orally administered once daily at night for 4 weeks. The outcome revealed significant reductions in both HbA1c and blood glucose levels. Furthermore, pancreatic insulin content significantly increased at a dose of 1 mg/kg. Urinary glucose excretion exhibited a dose-dependent increase, reaching significance at the 1 mg/kg dose¹.

溶解方案(细胞实验)

DMSO 中的溶解度 : ≥ 100 mg/mL (247.25 mM; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)|H₂O 中的溶解度 : < 0.1 mg/mL (insoluble)|* "≥" means soluble, but saturation unknown.

溶解方案(动物实验)

"方案 一": "请依序添加每种溶剂：10% DMSO 40% PEG300 5% Tween-80 45% SalineSolubility: ≥ 2.5 mg/mL (6.18 mM); 澄清溶液 此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水 定容至 1 mL。生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。"

"方案 二": "请依序添加每种溶剂：10% DMSO 90% (20% SBE-β-CD in Saline)Solubility: ≥ 2.5 mg/mL (6.18 mM); 澄清溶液 此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中，混合均匀。2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。"

"方案 三": "请依序添加每种溶剂：10% DMSO 90% Corn OilSolubility: ≥ 2.5 mg/mL (6.18 mM); 澄清溶液 此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。"