Tofogliflozin hydrate (CSG-452 hydrate) 是一种有效的，高度特异性的和选择性的SGLT2抑制剂，其IC50值为 2.9 nM，对人、大鼠和小鼠SGLT2的Ki值分别为 2.9 nM，14.9 nM 和 6.4 nM。Tofogliflozin hydrate 部分抑制肾小管细胞中高葡萄糖诱导的ROS生成。
| 生物活性 | Tofogliflozin hydrate (CSG-452 hydrate) is a potent and highly specificsodium/glucose cotransporter 2 (SGLT2)inhibitor with anIC50of 2.9 nM andKivalues of 2.9 nM, 14.9 nM, and 6.4 nM for human, rat, and mouseSGLT2[1]. Tofogliflozin partially inhibits high glucose-inducedreactive oxyen species (ROS)generation in tubular cells[2]. |
| IC50& Target | IC50: 2.9 nM (SGLT2); Ki: 2.9 nM ( humanSGLT2), 14.9 nM (ratSGLT2), and 6.4 nM (mouseSGLT2)[1] |
体外研究
(In Vitro) | Tofofloxacin (3-30 nM; 24 hours; tubular epithelial cells) treatment inhibits the oxidative stress generation and monocyte chemoattractant protein-1 (MCP-1) gene expression in tubular cells induced by high glucose[2].
Tofofloxacin (3-30 nM; 8 days; tubular epithelial cells) treatment inhibits the apoptotic cell death induced by high glucose[2].
RT-PCR[2] | Cell Line: | Tubular epithelial cells | | Concentration: | 3 nM and 30 nM | | Incubation Time: | 24 hours | | Result: | Inhibited MCP-1 gene expression in tubular cells induced by high glucose exposure. |
Apoptosis Analysis[2] | Cell Line: | Tubular epithelial cells | | Concentration: | 3 nM and 30 nM | | Incubation Time: | 8 days | | Result: | Inhibited the apoptotic cell death induced by high glucose. |
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体内研究
(In Vivo) | Tofogliflozin (0.1-10 mg/kg; oral administration; once daily; for 4 weeks;db/dbmice) treatment improves hyperglycemia and thereby ameliorated glucose intolerance of the obese diabetic mice[1].
| Animal Model: | db/dbmice[1] | | Dosage: | 0.1 mg/kg, 0.3 mg/kg, 1 mg/kg, 3 mg/kg, or 10 mg/kg | | Administration: | Oral administration; once daily; for 4 weeks | | Result: | Observed acute blood glucose reduction, dose-dependently reduced glycated hemoglobin, significantly prevented the decrease of IRI levels at doses of 3 and 10 mg/kg, and no difference in food intake or body weight. |
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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 : 0.33 mg/mL(0.82 mM;Need ultrasonic) *"≥" 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。 4. 请依序添加每种溶剂： PBS Solubility: 2.5 mg/mL (6.18 mM); Clear solution; Need ultrasonic and warming and heat to 60℃ *以上所有助溶剂都可在本网站选购。
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