Imeglimin
(Synonyms: EMD 387008) 目录号 : GC10576
Imeglimin (EMD 387008) 是一种口服降糖剂。
Cas No.:775351-65-0
Sample solution is provided at 25 µL, 10mM.
Imeglimin is the first antidiabetic compound that induces an increase in mitochondrial phospholipid composition, contributing to improvements in hepatic mitochondrial function.
Imeglimin also reduces reactive oxygen species production and increases mitochondrial DNA. Imeglimin effects on mitochondrial phospholipid composition can participate in the benefit of Imeglimin on mitochondrial function. Imeglimin increases mtDNA content without modifying PGC1α expression. Imeglimin amplifies the effects of high-fat, high-sucrose diet (HFHSD) on both cardiolipin and phosphatidylserine (PS) content, whereas it tends to restore phosphatidylcholine (PC), phosphatidylethanolamine (PE), and phosphatidylinositol (PI) content to normal values in HFHSD mitochondria[1].
Imeglimin is administered orally at 200 mg/kg b.i.d. during the last 6 weeks of the HFHSD feeding protocol. A slight decrease in body weight and food intake associated with some diarrhea is observed but only during the first few days of treatment. Imeglimin significantly decreases hyperglycemia, restores normal glucose tolerance, and improves insulin sensitivity[1].
References:
[1]. Vial G, et al. Imeglimin normalizes glucose tolerance and insulin sensitivity and improves mitochondrialfunction in liver of a high-fat, high-sucrose diet mice model. Diabetes. 2015 Jun;64(6):2254-64.
Kinase experiment: | Rotenone-sensitive NADH-ubiquinone oxidoreductase (complex I, CI) is assayed using 100 μM Decylubiquinone as an electron acceptor and 200 μM NADH as a donor in a 10 mM KH2PO4/K2HPO4 buffer, pH 7.5, containing 3.75 mg/mL BSA, 2 mM KCN, and 7.5 μM Antimycin A. NADH oxidation is measured at 340 nm before and after the addition of 4 μM Rotenone to allow the calculation of the Rotenone-sensitive-specific activity, which is characteristic of CI. Succinate-ubiquinone reductase (complex II, CII) activity is quantified by measuring the decrease in absorbance resulting from the reduction of 100 μM dichlorophenolindophenol at 600 nm. The measurement is performed in 50 mM KH2PO4/K2HPO4 buffer, pH 7.5, in the presence of 30 mM Succinate, 100 μM Decylubiquinone, 2 μM Rotenone, and 2 mM KCN. Coenzyme Q-cytochrome c-oxidoreductase activity (complex III, CIII), is quantified by measuring the increase in absorbance resulting from the reduction of 100 μM cytochrome c at 550 nm. The measurement is performed in 50 mM KH2PO4/K2HPO4 buffer, pH 7.5, in the presence of 100 μM Decylubiquinone previously reduced by dithionite, 50 μM EDTA, and 1 mM KCN. The specific activity is calculated by subtracting the activity obtained before and after addition of 5 μg/mL Antimycin A. 3-Hydroxyacyl-CoA dehydrogenase (HAD) activity is quantified by measuring the decrease in absorbance at 340 nm resulting from the oxidation of NADH (200 μM) and the reduction of S-acetoacetyl-CoA (50 μM). The measurement is performed in Imidazole (40 mM) and EDTA (60 μM), pH 7[1]. |
Animal experiment: | Mice[1]Male C57BL/6JOlaHsd mice at 4 weeks old are housed at 22°C with a 12-h light/dark cycle. After 1 week of acclimatization, 5-6-week-old mice are divided into two groups: one with free access to a standard chow diet (SD) and the other with free access to a pelleted HFHSD diet for 16 weeks. Animals receive Imeglimin 200 mg/kg b.i.d. by oral gavage during the last 6 weeks of HFHSD feeding. Control SD and HFHSD mice are treated by oral gavage with methylcellulose 0.5% as a vehicle for drug treatment (5 mL/kg). Food intake is measured every day during the first week and twice a week until the end of the experiment. Results are expressed as grams per day per mouse. |
References: [1]. Vial G, et al. Imeglimin normalizes glucose tolerance and insulin sensitivity and improves mitochondrialfunction in liver of a high-fat, high-sucrose diet mice model. Diabetes. 2015 Jun;64(6):2254-64. |
Cas No. | 775351-65-0 | SDF | |
别名 | EMD 387008 | ||
化学名 | (4R)-6-N,6-N,4-trimethyl-1,4-dihydro-1,3,5-triazine-2,6-diamine | ||
Canonical SMILES | CC1N=C(NC(=N1)N(C)C)N | ||
分子式 | C6H13N5 | 分子量 | 155.2 |
溶解度 | Soluble in DMSO | 储存条件 | Store at -20°C |
General tips | 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°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。 为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。 |
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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
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1 mg | 5 mg | 10 mg |
1 mM | 6.4433 mL | 32.2165 mL | 64.433 mL |
5 mM | 1.2887 mL | 6.4433 mL | 12.8866 mL |
10 mM | 0.6443 mL | 3.2216 mL | 6.4433 mL |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方) | ||||||||||
% DMSO % % Tween 80 % saline | ||||||||||
计算重置 |
计算结果:
工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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- Purity: >98.00%
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