1. Metabolic Enzyme/Protease Apoptosis Anti-infection
  2. Hexokinase Mitochondrial Metabolism Apoptosis Parasite
  3. Lonidamine

Lonidamine  (Synonyms: AF-1890; Diclondazolic Acid; DICA)

Cat. No.: HY-B0486 Purity: 99.73%
COA Handling Instructions

Lonidamine (AF-1890) is a hexokinase and mitochondrial pyruvate carrier inhibitor (Ki: 2.5 μM). Lonidamine also inhibits aerobic glycolysis in cancer cells. Lonidamine can be used in the research of mitochondrial metabolism and inflammation, such as pulmonary fibrosis.

For research use only. We do not sell to patients.

Lonidamine Chemical Structure

Lonidamine Chemical Structure

CAS No. : 50264-69-2

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 73 In-stock
Solution
10 mM * 1 mL in DMSO USD 73 In-stock
Solid
5 mg USD 66 In-stock
10 mg USD 79 In-stock
50 mg USD 158 In-stock
100 mg   Get quote  
200 mg   Get quote  

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 8 publication(s) in Google Scholar

Top Publications Citing Use of Products

    Lonidamine purchased from MedChemExpress. Usage Cited in: Cell Metab. 2022 Nov 11;S1550-4131(22)00490-9.  [Abstract]

    Combination treatment with Rimegepant and Lonidamine, Anlotinib, or Bevacizumab lead to a reduced proportion of Ki67+ cancer cells, reduce LC3B puncta, and the accumulation of p62 puncta in cancer cells, indicating impaired cell proliferation and autophagic flux.
    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Lonidamine (AF-1890) is a hexokinase and mitochondrial pyruvate carrier inhibitor (Ki: 2.5 μM). Lonidamine also inhibits aerobic glycolysis in cancer cells. Lonidamine can be used in the research of mitochondrial metabolism and inflammation, such as pulmonary fibrosis[1][2][3].

    IC50 & Target

    Ki: 2.5 μM (Mitochondrial pyruvate carrier)[2]

    In Vitro

    Lonidamine (100 μM, 24 h) inhibits TGF-β-stimulated lactate production and oxygen consumption rate in AKR-2B and TIG-1 cells[3].
    Lonidamine (100 μM, 24/48 h) inhibits H2030BrM3 and A549 cell proliferation[4].
    Lonidamine (100-200 μM, 24 h) inhibits H2030BrM3 and A549 cell invasion[4].
    Lonidamine (100-1000 μM, 24 h) inhibits mitochondrial complex I and II activities[4].
    Lonidamine (200 μM, 24 h) increases ROS generation in H2030BrM3 lung cancer cells[4].

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

    In Vivo

    Lonidamine (oral administration, 10-100 mg/kg/day, d10 to d20) improves lung function by inhibiting hexokinase 2 (HK2) activity in BLM-induced pulmonary fibrosis murine model[3].

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

    Animal Model: Lonidamine (oral administration, 10-100 mg/kg/day, d10 to d20) improves lung function by inhibiting hexokinase 2 (HK2) activity in BLM-induced pulmonary fibrosis murine model[3].
    Dosage: 10, 30, 100 mg/kg/day
    Administration: Oral administration, daily, d10 to d20 after BLM treatment.
    Result: Partially or completely reversed the increases in HK2 and lactate induced by BLM and reduced the expression of 10 profibrotic mediators.
    Clinical Trial
    Molecular Weight

    321.16

    Formula

    C15H10Cl2N2O2

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(C1=NN(CC2=CC=C(Cl)C=C2Cl)C3=C1C=CC=C3)O

    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 : 50 mg/mL (155.69 mM; Need ultrasonic; 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 3.1137 mL 15.5686 mL 31.1371 mL
    5 mM 0.6227 mL 3.1137 mL 6.2274 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)

    Mass
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    Volume
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    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

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    Volume (start)

    V1

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    C2

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    Volume (final)

    V2

    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    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.08 mg/mL (6.48 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

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

      Solubility: ≥ 2.08 mg/mL (6.48 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 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 (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

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

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    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: 99.73%

    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 3.1137 mL 15.5686 mL 31.1371 mL 77.8428 mL
    5 mM 0.6227 mL 3.1137 mL 6.2274 mL 15.5686 mL
    10 mM 0.3114 mL 1.5569 mL 3.1137 mL 7.7843 mL
    15 mM 0.2076 mL 1.0379 mL 2.0758 mL 5.1895 mL
    20 mM 0.1557 mL 0.7784 mL 1.5569 mL 3.8921 mL
    25 mM 0.1245 mL 0.6227 mL 1.2455 mL 3.1137 mL
    30 mM 0.1038 mL 0.5190 mL 1.0379 mL 2.5948 mL
    40 mM 0.0778 mL 0.3892 mL 0.7784 mL 1.9461 mL
    50 mM 0.0623 mL 0.3114 mL 0.6227 mL 1.5569 mL
    60 mM 0.0519 mL 0.2595 mL 0.5190 mL 1.2974 mL
    80 mM 0.0389 mL 0.1946 mL 0.3892 mL 0.9730 mL
    100 mM 0.0311 mL 0.1557 mL 0.3114 mL 0.7784 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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