Ipragliflozin (ASP1941) 是一种有效的，具有口服活性的选择性SGLT2抑制剂，对人 SGLT2 和 SGLT1，大鼠 SGLT2 和 SGLT1，小鼠 SGLT2 和 SGLT1 的IC50分别为 7.38 和 1876 nM，6.73 和 1166 nM，5.64 和 1380 nM。具有抗糖尿病活性。
| 生物活性 | Ipragliflozin (ASP1941) is an orally active and selectiveSGLT2inhibitor withIC50s of 7.38 and 1876 nM, 6.73 and 1166 nM, 5.64 and 1380 nM for humanSGLT2andSGLT1, ratSGLT2andSGLT1, mouseSGLT2andSGLT1, respectively. Antidiabetic agent[1]. |
| IC50& Target[1] | 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) |
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体外研究
(In Vitro) | Ipragliflozin (1-50 μM) significantly and dose-dependently suppresses the growth of MCF-7 human breast cancer cell lines.
Upon knocking down SGLT2 expression using siRNA, the attenuation of cell proliferation induced by Ipragliflozin is completely canceled, suggesting that Ipragliflozin attenuates breast cancer cell proliferation through SGLT2 inhibition.
BrdU assay revealed that Ipragliflozin at a high dose (50 and 100 μM) significantly inhibits DNA synthesis of MCF-7 cells[2].
Cell Viability Assay[2] | 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. |
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体内研究
(In Vivo) | Ipragliflozin shows antihyperglycemic effect. Ipragliflozin (0.1-1 mg/kg) dose-dependently inhibits increases in blood glucose levels. In STZ-induced type 1 diabetic rats, this effect is significant at doses of 0.3 and 1 mg/kg, and in KK-Aytype 2 diabetic mice, the effect is significant at all tested doses[1].
Ipragliflozin (0.3 and 1 mg/kg) shows antidiabetic effects of repeated administration in streptozotocin-induced type 1 diabetic rats[1].
| Animal Model: | Single Administration[1]
Streptozotocin (STZ; 50 mg/kg)-induced type 1 diabetic rats and KK-Aytype 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 Administration[1]
Streptozotocin (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 HbA1cand 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. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : ≥ 100 mg/mL(247.25 mM) H2O : ≥ 0.1 mg/mL(0.25 mM) *"≥" means soluble, but saturation unknown. 配制储备液 | 1 mM | 2.4725 mL | 12.3625 mL | 24.7249 mL | | 5 mM | 0.4945 mL | 2.4725 mL | 4.9450 mL | | 10 mM | 0.2472 mL | 1.2362 mL | 2.4725 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (6.18 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (6.18 mM，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；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (6.18 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (6.18 mM，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 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 3. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (6.18 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (6.18 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 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。 *以上所有助溶剂都可在本网站选购。
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