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Imeglimin hydrochloride

Antidiabetic agent CAS# 775351-61-6

Imeglimin hydrochloride

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Chemical structure

Imeglimin hydrochloride

3D structure

Chemical Properties of Imeglimin hydrochloride

Cas No. 775351-61-6 SDF Download SDF
PubChem ID 54763513 Appearance Powder
Formula C6H13N5 M.Wt 155.2
Type of Compound N/A Storage Desiccate at -20°C
Synonyms EMD 387008 hydrochloride
Solubility DMSO : 25 mg/mL (130.44 mM; Need ultrasonic)
Chemical Name (4R)-6-N,6-N,4-trimethyl-1,4-dihydro-1,3,5-triazine-2,6-diamine;hydrochloride
SMILES CC1N=C(NC(=N1)N(C)C)N.Cl
Standard InChIKey UXHLCYMTNMEXKZ-PGMHMLKASA-N
Standard InChI InChI=1S/C6H13N5.ClH/c1-4-8-5(7)10-6(9-4)11(2)3;/h4H,1-3H3,(H3,7,8,9,10);1H/t4-;/m1./s1
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of Imeglimin hydrochloride

DescriptionImeglimin hydrochloride is the first antidiabetic compound that induces an increase in mitochondrial phospholipid composition, contributing to improvements in hepatic mitochondrial function.In Vitro: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].In Vivo: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.

Protocol

Kinase Assay [1]
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 Administration [1]
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.

Imeglimin hydrochloride Dilution Calculator

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Imeglimin hydrochloride Molarity Calculator

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Preparing Stock Solutions of Imeglimin hydrochloride

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 6.4433 mL 32.2165 mL 64.433 mL 128.866 mL 161.0825 mL
5 mM 1.2887 mL 6.4433 mL 12.8866 mL 25.7732 mL 32.2165 mL
10 mM 0.6443 mL 3.2216 mL 6.4433 mL 12.8866 mL 16.1082 mL
50 mM 0.1289 mL 0.6443 mL 1.2887 mL 2.5773 mL 3.2216 mL
100 mM 0.0644 mL 0.3222 mL 0.6443 mL 1.2887 mL 1.6108 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on Imeglimin hydrochloride

AMP-activated protein kinase (AMPK) acts as an integrator of regulatory signals to monitor systemic and cellular energy status. Imeglimin targets on three main organs involved in glucose homeostasis: liver, muscle and the pancreas and thus has a distinct mode of action in comparison to existing Type 2 diabetes treatments.
In vitro: In liver mitochondria, imeglimin redirects substrate flows in favor of complex II. Moreover, imeglimin inhibits complex I and restores complex III activities, advicing an increase of fatty acid oxidation, further supported by an increase in hepatic 3-hydroxyacetyl-CoA dehydrogenase activity and acylcarnitine profile. Imeglimin was also found to reduce the production of reactive oxygen species and increases the DNA of mitochondrial [1].
In vivo: A previous study used a model of 16-week high-fat, high-sucrose diet (HFHSD) mice to characterize imeglimin’s antidiabetic effects. Six-week imeglimin treatment could decrease glycemia, restore normal glucose tolerance, and improve insulin sensitivity, body weights and food intake significantly. This was associated with an increase of insulin-stimulated protein kinase B phosphorylation in the liver and muscle. In conclusion, imeglimin could normalize glucose tolerance and insulin sensitivity via preserving mitochondrial function from oxidative stress and favoring lipid oxidation in liver of HFHSD mice [1].
Clinical trial: Imeglimin is an experimental drug being developed as an oral anti-diabetic. Imeglimin is in development (completed phase IIb clinical trials) for use both as monotherapy and in combination with other type-2 diabetes treatments. Various research protocols are being known through various scientists. Early studies showed that imeglimin is as effective as metformin in regulating glycaemic control.
Reference:
[1] Vial G, Chauvin MA, Bendridi N, Durand A, Meugnier E, Madec AM, Bernoud-Hubac N, Pais de Barros JP, Fontaine É, Acquaviva C, Hallakou-Bozec S, Bolze S, Vidal H, Rieusset J.Imeglimin Normalizes Glucose Tolerance and Insulin Sensitivity and Improves Mitochondrial Function in Liver of a High-Fat High-Sucrose Diet Mice Model. Diabetes. 2014. pii: db141220

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Description

Imeglimin hydrochloride (EMD 387008) is an oral glucose-lowering agent. Imeglimin also reduces reactive oxygen species (ROS) production, increases mitochondrial DNA and improves mitochondrial function.

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