1. Membrane Transporter/Ion Channel
  2. Na+/K+ ATPase
  3. Bufalin

Bufalin is an active component isolated from Chan Su, acts as a potent Na+/K+-ATPase inhibitor, binds to the subunit α1, α2 and α3, with Kd of 42.5, 45 and 40 nM, respectively. Anti-cancer activity.

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

Bufalin Chemical Structure

Bufalin Chemical Structure

CAS No. : 465-21-4

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 77 In-stock
Solution
10 mM * 1 mL in DMSO USD 77 In-stock
Solid
5 mg USD 70 In-stock
10 mg USD 100 In-stock
50 mg   Get quote  
100 mg   Get quote  

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Customer Review

Based on 7 publication(s) in Google Scholar

Top Publications Citing Use of Products

    Bufalin purchased from MedChemExpress. Usage Cited in: Apoptosis. 2023 May 30.  [Abstract]

    Bufalin (12.5, 25, 50, 100, 200 nM; 24, 48, 72 h) significantly reduces the viability of MKN-45 and HGC-27 GC cells in a dose- and time-dependent manner.
    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Bufalin is an active component isolated from Chan Su, acts as a potent Na+/K+-ATPase inhibitor, binds to the subunit α1, α2 and α3, with Kd of 42.5, 45 and 40 nM, respectively[1][2]. Anti-cancer activity[2].

    IC50 & Target

    Kd: 42.5 nM (Na,K-ATPase α1), 45 nM (Na,K-ATPase α2), 40 nM (Na,K-ATPase α3)[1]

    In Vitro

    Bufalin (0, 1, 2, 4 μM for 48 hours) decreases cell viability in NCI-H460 cells[2].
    Bufalin (2 μM) increases caspae-3, Endo G and GADD153 mRNA expression, but decreases the GRP78 mRNA expression[2].

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

    Cell Viability Assay[2]

    Cell Line: NCI-H460 cells
    Concentration: 0, 1, 2, 4 μM
    Incubation Time: 48 hours
    Result: Decreased viability of NCI-H460 cells in a dose-dependent manner.
    In Vivo

    Bufalin (0.1, 0.2, or 0.4 mg/kg, i.p., daily for 14 days) shows significant anti-tumor activity in mice bearing NCI-H460 cells[2].

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

    Animal Model: Forty male athymic BALB/c nu/nu mice (6-8 weeks old)[2]
    Dosage: 0.1, 0.2, or 0.4 mg/kg
    Administration: I.P. every day until 14 days
    Result: Dose-dependently suppressed tumor growth.
    Molecular Weight

    386.52

    Formula

    C24H34O4

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O[C@]([C@@](CC[C@@]1([H])[C@@]2(CC[C@H](O)C1)C)([H])[C@]2([H])CC3)(CC[C@@H]4C(C=C5)=COC5=O)[C@]34C

    Structure Classification
    Initial Source

    toad

    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 : 100 mg/mL (258.72 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 2.5872 mL 12.9359 mL 25.8719 mL
    5 mM 0.5174 mL 2.5872 mL 5.1744 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

    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    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (6.47 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 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: ≥ 2.5 mg/mL (6.47 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)

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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:
    %
    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: 99.86%

    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 2.5872 mL 12.9359 mL 25.8719 mL 64.6797 mL
    5 mM 0.5174 mL 2.5872 mL 5.1744 mL 12.9359 mL
    10 mM 0.2587 mL 1.2936 mL 2.5872 mL 6.4680 mL
    15 mM 0.1725 mL 0.8624 mL 1.7248 mL 4.3120 mL
    20 mM 0.1294 mL 0.6468 mL 1.2936 mL 3.2340 mL
    25 mM 0.1035 mL 0.5174 mL 1.0349 mL 2.5872 mL
    30 mM 0.0862 mL 0.4312 mL 0.8624 mL 2.1560 mL
    40 mM 0.0647 mL 0.3234 mL 0.6468 mL 1.6170 mL
    50 mM 0.0517 mL 0.2587 mL 0.5174 mL 1.2936 mL
    60 mM 0.0431 mL 0.2156 mL 0.4312 mL 1.0780 mL
    80 mM 0.0323 mL 0.1617 mL 0.3234 mL 0.8085 mL
    100 mM 0.0259 mL 0.1294 mL 0.2587 mL 0.6468 mL
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    Bufalin 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.

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    Product Name:
    Bufalin
    Cat. No.:
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