1. Metabolic Enzyme/Protease
  2. Mitochondrial Metabolism
  3. CTPI-2

CTPI-2 is a third-generation mitochondrial citrate carrier SLC25A1 inhibitor with a KD of 3.5 μM. CTPI-2 inhibits glycolysis, PPARγ, and its downstream target the glucose transporter GLUT4. CTPI-2 halts salient alterations of NASH reverting steatosis, preventing the evolution to steatohepatitis, reducing inflammatory macrophage infiltration in the liver and adipose tissue, and starkly mitigating obesity induced by a high-fat diet. Antitumor activity.

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CAS No. : 68003-38-3

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Customer Review

Based on 13 publication(s) in Google Scholar

Top Publications Citing Use of Products

    CTPI-2 purchased from MedChemExpress. Usage Cited in: Int J Oncol. 2025 Feb;66(2):15.  [Abstract]

    Migration ability of ESCC cells treated with CTPI-2 (30 μM) was detected via a wound healing assay.

    CTPI-2 purchased from MedChemExpress. Usage Cited in: Redox Biol. 2024 May 9:73:103187.  [Abstract]

    ROS production by MDDCs labeled with 2′,7′-dichlorofluorescein diacetate and stimulated for 30 min with zymosan in the presence of 10 μM CTPI-2. Results are expressed as per cent values of zymosan effect.

    CTPI-2 purchased from MedChemExpress. Usage Cited in: EMBO J. 2022 Apr 19;41(8):e109463.  [Abstract]

    Effect of 10 μM CTPI-2 on the expression of cytokine mRNA.

    CTPI-2 purchased from MedChemExpress. Usage Cited in: EMBO J. 2022 Apr 19;41(8):e109463.  [Abstract]

    Assay of cytokine protein expression in the supernatants of MDDCs stimulated overnight with zymosan in the presence and absence of CTPI-2.

    CTPI-2 purchased from MedChemExpress. Usage Cited in: EMBO J. 2022 Apr 19;41(8):e109463.  [Abstract]

    The effects of CTPI-2 (50 mg/kg, i.p.) on HSC expansion in the early phase after the administration of 5-FU. Numbers in the dot plots represent the frequencies of the indicated fractions within total BM cells.
    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    CTPI-2 is a third-generation mitochondrial citrate carrier SLC25A1 inhibitor with a KD of 3.5 μM. CTPI-2 inhibits glycolysis, PPARγ, and its downstream target the glucose transporter GLUT4. CTPI-2 halts salient alterations of NASH reverting steatosis, preventing the evolution to steatohepatitis, reducing inflammatory macrophage infiltration in the liver and adipose tissue, and starkly mitigating obesity induced by a high-fat diet. Antitumor activity[1][2].

    IC50 & Target

    KD: 3.5 μM (SLC25A1)[1]

    In Vivo

    CTPI-2 is a unique regulator of glycolysis that limits the metabolic plasticity of cancer stem cells (CSCs). CTPI-2 (26 mg/kg; i.p.) inhibits tumor growth in in vivo models of non-small cell lung cancer (NSCLC)[1].
    CTPI-2 (50 mg/kg; i.p.; alternate days for 12 weeks) completely averts weight gain in the prevention study and leads to significant weight loss in the reversion study[2].
    CTPI-2 prevents steatohepatitis and normalizes glucose tolerance. CTPI-2 lowers the levels of circulating IL-6 while increasing anti-inflammatory IL-4 and IL-10 and also reduced the monocyte chemoattractant protein-1 and monokine-induced by interferon-γ that attract neutrophils and monocytes. CTPI-2 regulates the citrate pool, the lipogenic and the gluconeogenic pathways[2].

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

    Animal Model: C57BL/6J mice (HFD-fed mice)[2]
    Dosage: 50 mg/kg
    Administration: Alternate days via the intraperitoneal route for 12 weeks
    Result: Completely averted weight gain in the prevention study and led to significant weight loss in the reversion study.
    Molecular Weight

    356.74

    Formula

    C13H9ClN2O6S

    CAS No.
    Appearance

    Solid

    Color

    Off-white to light yellow

    SMILES

    O=C(O)C1=CC=CC=C1NS(=O)(C2=CC=C(Cl)C([N+]([O-])=O)=C2)=O

    Shipping

    Room temperature in continental US; may vary elsewhere.

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

    DMSO : 116.67 mg/mL (327.04 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 2.8032 mL 14.0158 mL 28.0316 mL
    5 mM 0.5606 mL 2.8032 mL 5.6063 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    • 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

    Concentration (start)

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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    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.08 mg/mL (5.83 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% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.08 mg/mL (5.83 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 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.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

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    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: 99.99%

    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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.8032 mL 14.0158 mL 28.0316 mL 70.0791 mL
    5 mM 0.5606 mL 2.8032 mL 5.6063 mL 14.0158 mL
    10 mM 0.2803 mL 1.4016 mL 2.8032 mL 7.0079 mL
    15 mM 0.1869 mL 0.9344 mL 1.8688 mL 4.6719 mL
    20 mM 0.1402 mL 0.7008 mL 1.4016 mL 3.5040 mL
    25 mM 0.1121 mL 0.5606 mL 1.1213 mL 2.8032 mL
    30 mM 0.0934 mL 0.4672 mL 0.9344 mL 2.3360 mL
    40 mM 0.0701 mL 0.3504 mL 0.7008 mL 1.7520 mL
    50 mM 0.0561 mL 0.2803 mL 0.5606 mL 1.4016 mL
    60 mM 0.0467 mL 0.2336 mL 0.4672 mL 1.1680 mL
    80 mM 0.0350 mL 0.1752 mL 0.3504 mL 0.8760 mL
    100 mM 0.0280 mL 0.1402 mL 0.2803 mL 0.7008 mL
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    Help & FAQs
    • 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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    Product Name:
    CTPI-2
    Cat. No.:
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