Dapagliflozin (BMS-512148) 是一种竞争性葡萄糖协同转运蛋白2 (SGLT2) 抑制剂,可导致尿液中葡萄糖的排泄,用于糖尿病 (DM) 的研究。Dapagliflozin 诱导HIF1表达并减轻肾脏 IR 损伤。
生物活性 | Dapagliflozin (BMS-512148), a new type of drug used to treat diabetes mellitus (DM), is a competitive sodium/glucose cotransporter 2 (SGLT2) inhibitor, which results in excretion of glucose into the urine[1].
Dapagliflozin inducesHIF1expression and attenuates renal IR injury[2]. |
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体外研究 (In Vitro) | Dapagliflozin (0-10 μM;24 hours) significantly increases the cell survival in hypoxic HK2 cell in a dose-dependent manner[2].Dapagliflozin (0-10 μM;2 hours) increases the HIF1 expression, increases AMPK and EKR phosphorylation in hypoxic HK2 cells, but shows no effect on the phosphorylation of AMPK and ERK in normoxic HK2 cells[2]..
Cell Viability Assay[1] Cell Line: | Hypoxic HK2 cells | Concentration: | 0 μM, 1 μM, 2 μM, 5 μM, 10 μM | Incubation Time: | 24 hours | Result: | Improved the cell viability in a dose-dependent manner compared with control cells. |
Western Blot Analysis[1] Cell Line: | Hypoxic HK2 cells, Normoxic HK2 cells | Concentration: | 0 μM, 1 μM, 2 μM, 5 μM, 10 μM | Incubation Time: | 24 hours | Result: | Induced HIF1 expression in hypoxic and normoxic HK2 cells. |
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体内研究 (In Vivo) | Dapagliflozin (oral administration; 10 mg/kg) causes a marked increase in urinary glucose in SGLT2i-mice, suppresses BAT thermogenesis by reducing sympathetic nerve activity and enhances hepatic gluconeogenesis and glycogenolysis[3].
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
溶解性数据 | In Vitro: DMSO : ≥ 100 mg/mL(244.58 mM) H2O : 50 mg/mL(122.29 mM;Need ultrasonic) *"≥" means soluble, but saturation unknown. 配制储备液 1 mM | 2.4458 mL | 12.2288 mL | 24.4577 mL | 5 mM | 0.4892 mL | 2.4458 mL | 4.8915 mL | 10 mM | 0.2446 mL | 1.2229 mL | 2.4458 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 (sealed storage, away from moisture)。-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: PBS Solubility: 33.33 mg/mL (81.52 mM); Clear solution; Need ultrasonic and warming and heat to 60℃ 2. 请依序添加每种溶剂: 5% DMSO 40%PEG300 5%Tween-80 50% saline Solubility: ≥ 2.5 mg/mL (6.11 mM); Clear solution 3. 请依序添加每种溶剂: 5% DMSO 95% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (6.11 mM); Clear solution 4. 请依序添加每种溶剂: 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.08 mg/mL (5.09 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (5.09 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 20.8 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。 5. 请依序添加每种溶剂: 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.08 mg/mL (5.09 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (5.09 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 20.8 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。 6. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 2.08 mg/mL (5.09 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (5.09 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 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。 7. 请依序添加每种溶剂: 1% DMSO 99% saline Solubility: ≥ 0.5 mg/mL (1.22 mM); Clear solution *以上所有助溶剂都可在本网站选购。
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