1. Membrane Transporter/Ion Channel Apoptosis
  2. GLUT Apoptosis
  3. Glutor

Glutor is a selective GLUT 1/2/3 inhibitor that can suppress glucose uptake. Glutor can inhibit glycolysis and has anti-tumor activity, inducing cell apoptosis.

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Glutor Chemical Structure

Glutor Chemical Structure

CAS No. : 2561471-22-3

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Based on 1 publication(s) in Google Scholar

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Description

Glutor is a selective GLUT 1/2/3 inhibitor that can suppress glucose uptake. Glutor can inhibit glycolysis and has anti-tumor activity, inducing cell apoptosis[1][2].

In Vitro

Glutor reduced the uptake of 2-DG with similar efficacy in different cancer cell lines, such as HCT116 (IC50 = 10.8 nM), UM-UC-3 (IC50 = 8.3 nM), UO-31 (IC50 = 3.6 nM), and MIA PaCa-2 (IC50 = 1.1 nM)[1].
Glutor effectively decreases glycolysis in HCT116 cells, thereby preventing the reduction of oxidative phosphorylation rates after glucose addition[1].
Glutor inhibits the proliferation of malignant cell lines without harming the growth of non-malignant peripheral blood mononuclear cells (PBMCs) and IMR-90 embryonic lung cells[1].
Glutor (0.5μM, 24-48h) suppresses the glucose uptake-induced upregulation of GLUT-1 and GLUT-3 expression[1].
Glutor (0.0001-1μM, 24h) inhibits the number of DL cells in a time- and dose-dependent manner, with an Glutor reduced the uptake of 2-DG with similar efficacy in different cancer cell lines, such as HCT116 (IC50 = 10.8 nM), UM-UC-3 (IC50 = 8.3 nM), UO-31 (IC50 = 3.6 nM), and MIA PaCa-2 (IC50 = 1.1 nM)[1].
Glutor effectively decreases glycolysis in HCT116 cells, thereby preventing the reduction of oxidative phosphorylation rates after glucose addition[1].
Glutor inhibits the proliferation of malignant cell lines without harming the growth of non-malignant peripheral blood mononuclear cells (PBMCs) and IMR-90 embryonic lung cells[1].
Glutor (0.5 μM, 24-48 h) suppresses the glucose uptake-induced upregulation of GLUT-1 and GLUT-3 expression[1].
Glutor (0.0001-1 μM, 24 h) inhibits the number of DL cells in a time- and dose-dependent manner, with an IC50 of 0.01 μM, showing no cytotoxicity to thymocytes[2].
Glutor (0.01-1 μM, 24 h) induces apoptosis in DL cells[2].
Glutor (0.01-1 μM, 24 h) links tumor inhibition to the regulation of cell survival and metabolic regulatory molecules[2].
Glutor (0.01-1 μM, 2 h) increases the expression of reactive oxygen species (ROS) in DL cells[2].
Glutor (0.01-1 μM, 24 h) triggers depolarization of the mitochondrial membrane, disrupting the pH homeostasis of DL cells and altering their chemical sensitivity[2].
of 0.01 μM, showing no cytotoxicity to thymocytes[2].
Glutor (0.01-1 μM, 24 h) induces apoptosis in DL cells[2].
Glutor (0.01-1 μM, 24 h) links tumor inhibition to the regulation of cell survival and metabolic regulatory molecules[2].
Glutor (0.01-1 μM, 2 h) increases the expression of reactive oxygen species (ROS) in DL cells[2].
Glutor (0.01-1 μM, 24 h) triggers depolarization of the mitochondrial membrane, disrupting the pH homeostasis of DL cells and altering their chemical sensitivity[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Real Time qPCR[1]

Cell Line: DLD-1
Concentration: 0.5 μM
Incubation Time: 24, 48 h
Result: Showed under low blood sugar conditions, the levels of GLUT1 and GLUT3 increase.

Western Blot Analysis[1]

Cell Line: DLD-1
Concentration: 0.5 μM
Incubation Time: 24, 48 h
Result: Showed under low blood sugar conditions, the levels of GLUT1 and GLUT3 increase.

Cell Viability Assay[2]

Cell Line: DL
Concentration: 0.0001, 0.001, 0.01, 0.1, 1μM
Incubation Time: 24 h
Result: Showed the number of cells decreases in a dose- and time-dependent manner.

Apoptosis Analysis[2]

Cell Line: DL
Concentration: 0.01 μM
Incubation Time: 24 h
Result: Increased the number of cells with typical apoptotic morphological characteristics.

Western Blot Analysis[2]

Cell Line: DL
Concentration: 0.01 μM
Incubation Time: 24 h
Result: Suppressed the expression of hypoxia-inducible factor 1-alpha (HIF-1a), hexokinase 2 (HK-2), and lactate dehydrogenase A (LDH-A), regulating the expression of cell survival molecules B-cell lymphoma 2 (Bcl-2), Bcl-2-associated X (BAX), and p53. The expression of Bcl-2, transforming growth factor-beta (TGF-b), Cmyc, and heat shock protein 70 (Hsp70) decreased, while the expression of BAX and p53 increased.
Molecular Weight

536.62

Formula

C31H32N6O3

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C([C@@]1(C)N(C(C2=CC(C3=CC=CC=C3)=NN2C1)=O)CC(C=C4)=CC=C4N5CCOCC5)NCC6=CC=CN=C6

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 34 mg/mL (63.36 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8635 mL 9.3176 mL 18.6352 mL
5 mM 0.3727 mL 1.8635 mL 3.7270 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 5 mg/mL (9.32 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 5 mg/mL (9.32 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.54%

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.8635 mL 9.3176 mL 18.6352 mL 46.5879 mL
5 mM 0.3727 mL 1.8635 mL 3.7270 mL 9.3176 mL
10 mM 0.1864 mL 0.9318 mL 1.8635 mL 4.6588 mL
15 mM 0.1242 mL 0.6212 mL 1.2423 mL 3.1059 mL
20 mM 0.0932 mL 0.4659 mL 0.9318 mL 2.3294 mL
25 mM 0.0745 mL 0.3727 mL 0.7454 mL 1.8635 mL
30 mM 0.0621 mL 0.3106 mL 0.6212 mL 1.5529 mL
40 mM 0.0466 mL 0.2329 mL 0.4659 mL 1.1647 mL
50 mM 0.0373 mL 0.1864 mL 0.3727 mL 0.9318 mL
60 mM 0.0311 mL 0.1553 mL 0.3106 mL 0.7765 mL
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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