2. Membrane Transporter/Ion Channel
  3. Na+/Ca2+ Exchanger
  4. CGP37157

CGP37157 is a potent, selective inhibitor of Na+/Ca2+ exchanger, inhibiting the Na+-induced Ca2+-release from guinea-pig heart mitochondria, with an IC50 of 0.8 μM.

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CAS No. : 75450-34-9

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Customer Review

Based on 9 publication(s) in Google Scholar

CGP37157 Related Antibodies

Top Publications Citing Use of Products

    CGP37157 purchased from MedChemExpress. Usage Cited in: Nature. 2024 Jul;631(8022):826-834.  [Abstract]

    [Ca2+]i changes of primary cultured cortical neurons imaged from Asic1a+/+ mice (n = 20–26 cells from 3 cultures per group). 200 μM glutamate, 10 μM LY341495 (mGluRs blockers), 10 μM CGP37157 (inhibitor of Na+/Ca2+ exchanger in mitochondria), 10 μM RO2959 (selective Ca2+ release-activated Ca2+ channel inhibitor) and 100 ng/ml PcTX-1 were applied.

    CGP37157 purchased from MedChemExpress. Usage Cited in: Cell Res. 2022 Jul;32(7):638-658.  [Abstract]

    OCR measurement. HUVECs were treated with R-2-HG (10 mM) plus CGP-37157 (10 μM) for 1 h.

    CGP37157 purchased from MedChemExpress. Usage Cited in: Cell Res. 2022 Jul;32(7):638-658.  [Abstract]

    Aortic ring sprouting assay. Matrigel-ring mixture was treated with R-2-HG (10 mM) plus CGP-37157 (10 μM) for 7 days.

    CGP37157 purchased from MedChemExpress. Usage Cited in: Cell Res. 2022 Jul;32(7):638-658.  [Abstract]

    The impact of the mitochondrial respiration, Na+/Ca2+ exchange and R-2-HG uptake on F-actin formation. HUVECs were treated with R-2-HG (10 mM) alone or in combination with CGP-37157 (10 μM) for 1 h.

    CGP37157 purchased from MedChemExpress. Usage Cited in: Cell Res. 2022 Jul;32(7):638-658.  [Abstract]

    R-2-HG-induced mitochondrial migration in HUVECs. Cells were treated with R-2-HG (10 mM) and CGP-37157 (10 μM) at the indicated time-points. Mitochondria were visualized by MitoTracker Red. Shown were snapshots of fluorescence images of time-lapse videos of mitochondrial redistribution.

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    CGP37157 is a potent, selective inhibitor of Na+/Ca2+ exchanger, inhibiting the Na+-induced Ca2+-release from guinea-pig heart mitochondria, with an IC50 of 0.8 μM.

    IC50 & Target

    IC50: 0.8 μM (Na+/Ca2+ exchanger)[1]
    In Vitro

    CGP37157 (Compound XVI) is a potent, selective inhibitor of Na+/Ca2+ exchanger, inhibiting the Na+-induced Ca2+-release from guinea-pig heart mitochondria, with an IC50 of 0.8 μM[1].
    CGP37157 (10 μM) shows inhibitory effect on mitochondrial Na+/Ca2+ exchanger in cortical neurons, modulates intracellular Ca2+ levels via suppresssing voltage-gated calcium channels, and reduces NMDA-induced cytosolic and mitochondrial Ca2+ overloads. CGP37157 (10 μM) also reduces NMDA-induced excitotoxicity, and such an effect is via attenuating mitochondrial damage and calpain activity in neurons[2].
    CGP37157 (10 μM) in combination with salinomycin significantly attenuates cell viability and increases apoptosis of FaDu and HLaC79 cells. Moreover, CGP37157 has no inhibitory effect on salinomycin tumor toxicity[3].

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

    CGP37157 Related Antibodies
    Molecular Weight

    324.22

    Formula

    C15H11Cl2NOS
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C1NC2=CC=C(Cl)C=C2C(C3=CC=CC=C3Cl)SC1
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 125 mg/mL (385.53 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 3.0843 mL 15.4214 mL 30.8428 mL
    5 mM 0.6169 mL 3.0843 mL 6.1686 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
    =
    Concentration
    ×
    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

    ×
    Volume (start)

    V1

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    Concentration (final)

    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: ≥ 2.5 mg/mL (7.71 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (7.71 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 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 (25.0 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
    References
    Cell Assay
    [1]

    Cell toxicity assays are performed. Neurons are exposed to NMDA in HBSS (free of Ca2+ and Mg2+) containing 2.6 mM CaCl2, 10 mM glucose and 10 μM glycine for 10 or 30 min at 37°C, depending on the experiment. CGP37157 is present before and during the excitotoxic insult and cell viability is assessed 24 h later using Citotox 96 colorimetric assay. All experiments are performed in quadruplicate and the values provided are the normalized mean ± S.E.M. of at least three independent experiments[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 3.0843 mL 15.4214 mL 30.8428 mL 77.1070 mL
    5 mM 0.6169 mL 3.0843 mL 6.1686 mL 15.4214 mL
    10 mM 0.3084 mL 1.5421 mL 3.0843 mL 7.7107 mL
    15 mM 0.2056 mL 1.0281 mL 2.0562 mL 5.1405 mL
    20 mM 0.1542 mL 0.7711 mL 1.5421 mL 3.8553 mL
    25 mM 0.1234 mL 0.6169 mL 1.2337 mL 3.0843 mL
    30 mM 0.1028 mL 0.5140 mL 1.0281 mL 2.5702 mL
    40 mM 0.0771 mL 0.3855 mL 0.7711 mL 1.9277 mL
    50 mM 0.0617 mL 0.3084 mL 0.6169 mL 1.5421 mL
    60 mM 0.0514 mL 0.2570 mL 0.5140 mL 1.2851 mL
    80 mM 0.0386 mL 0.1928 mL 0.3855 mL 0.9638 mL
    100 mM 0.0308 mL 0.1542 mL 0.3084 mL 0.7711 mL
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    CGP37157 Related Classifications

    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.

    Keywords:

    CGP3715775450-34-9CGP 37157CGP-37157Na+/Ca2+ ExchangerInhibitorinhibitorinhibit

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