Home>>Signaling Pathways>> Proteases>> Mitochondrial Metabolism>>Imeglimin hydrochloride

Imeglimin hydrochloride

Catalog No.GC10956

Antidiabetic agent

Products are for research use only. Not for human use. We do not sell to patients.

Imeglimin hydrochloride Chemical Structure

Cas No.: 775351-61-6

Size Price Stock Qty
5mg
$88.00
In stock
10mg
$140.00
In stock
50mg
$419.00
In stock
100mg
$1,207.00
In stock

Tel:(909) 407-4943 Email: sales@glpbio.com

Customer Reviews

Based on customer reviews.

  • GlpBio Citations

    GlpBio Citations
  • Bioactive Compounds Premium Provider

    Bioactive Compounds Premium Provider

Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

View current batch:

Protocol

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.

Background

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

Chemical Properties

Cas No. 775351-61-6 SDF
Chemical Name (R)-6-imino-N,N,4-trimethyl-1,4,5,6-tetrahydro-1,3,5-triazin-2-amine hydrochloride
Canonical SMILES C[C@](N=C(N(C)C)N1)([H])NC1=N.Cl
Formula C6H14ClN5 M.Wt 191.66
Solubility ≥ 29.9mg/mL in DMSO Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

Prepare stock solution
1 mg 5 mg 10 mg
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
  • Molarity Calculator

  • Dilution Calculator

Mass
=
Concentration
x
Volume
x
MW*
 
 
 
**When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / CoA (available online).

Calculate

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

Reviews

Review for Imeglimin hydrochloride

Average Rating: 5 ★★★★★ (Based on Reviews and 9 reference(s) in Google Scholar.)

5 Star
100%
4 Star
0%
3 Star
0%
2 Star
0%
1 Star
0%
Review for Imeglimin hydrochloride

GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.

Required fields are marked with *

You may receive emails regarding this submission. Any emails will include the ability to opt-out of future communications.