Imeglimin hydrochloride (EMD 387008 hydrochloride) 是一种口服降糖剂。Imeglimin 可改善胰岛素敏感性。Imeglimin 还减少活性氧 (ROS) 的产生,增加了线粒体 DNA,并改善线粒体功能。
生物活性 | Imeglimin hydrochloride (EMD 387008) is an oral glucose-lowering agent. Imeglimin also reducesreactive oxygen species(ROS) production, increases mitochondrial DNA and improvesmitochondrialfunction[1]. |
IC50& Target | ROS; mitochondrial function[1] |
体外研究 (In Vitro) | Preincubation with Imeglimin (10 mM for 4 h or 100 μM for 24 h) also fully prevented tert-butylhydroperoxide (tBH)-induced cell death[2].
Cell Viability Assay[2] Cell Line: | Human endothelial cells (HMEC-1) | Concentration: | 100 μM and10 mM | Incubation Time: | 100 μM for 24 h, 10 mM for 4 h | Result: | Prevention of cell death. |
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体内研究 (In Vivo) | Imeglimin (200 mg/kg b.i.d. by oral gavage during the last 6 weeks of HFHSD feeding) significantly decreases hyperglycemia, and restores normal glucose tolerance[1].
Animal Model: | Male C57BL/6JOlaHsd mice (4 weeks old)[1] | Dosage: | 200 mg/kg | Administration: | Oral gavage; b.i.d.; 6 weeks | Result: | A slight decrease in body weight and food intake associated with some diarrhea was observed but only during the first few days of treatment. |
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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: H2O : ≥ 50 mg/mL(260.88 mM) DMSO : 25 mg/mL(130.44 mM;Need ultrasonic) *"≥" means soluble, but saturation unknown. 配制储备液 1 mM | 5.2176 mL | 26.0879 mL | 52.1757 mL | 5 mM | 1.0435 mL | 5.2176 mL | 10.4351 mL | 10 mM | 0.5218 mL | 2.6088 mL | 5.2176 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: 100 mg/mL (521.76 mM); Clear solution; Need ultrasonic 2. 请依序添加每种溶剂: 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.08 mg/mL (10.85 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (10.85 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。 3. 请依序添加每种溶剂: 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.08 mg/mL (10.85 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (10.85 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。 4. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 2.08 mg/mL (10.85 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (10.85 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。 *以上所有助溶剂都可在本网站选购。
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