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

Oleandrin  (Synonyms: PBI-05204)

Cat. No.: HY-13719 Purity: 99.93%
COA Handling Instructions

Oleandrin (PBI-05204) inhibits the Na+, K+-ATPase activity with an IC50 of 620 nM.

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

Oleandrin Chemical Structure

Oleandrin Chemical Structure

CAS No. : 465-16-7

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 444 In-stock
10 mM * 1 mL in DMSO USD 444 In-stock
2 mg USD 180 In-stock
5 mg USD 350 In-stock
10 mg USD 560 In-stock
25 mg USD 1122 In-stock
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Customer Review

Based on 3 publication(s) in Google Scholar

Top Publications Citing Use of Products

    Oleandrin purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2020 Apr;124:109852.  [Abstract]

    MCF7 and MDA-MB-231 cells are treated with Oleandrin or DMSO for 24 h. The expression of Bcl-2, Bim, and Bax is detected by western blot using β-actin as a loading control.
    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review


    Oleandrin (PBI-05204) inhibits the Na+, K+-ATPase activity with an IC50 of 620 nM.

    IC50 & Target

    IC50: 620 nM (Na+, K+-ATPase)[1].

    In Vitro

    Study of Na,K-ATPase inhibition shows an IC50 (nM) of 620 for Oleandrin. The inhibition of Na,K-ATPase by Oleandrin confirms that it likely exert its toxic effect through inhibition of sodium pump activity[1]. When treated with a series of concentrations of Oleandrin (0.2-25 nM), the undifferentiated CaCO-2 cells are sensitive as evidenced by an IC50 of 8.25 nM. In contrast, a maximum growth inhibition of only 20% is reached in differentiated CaCO-2 cells even though they are treated with Oleandrin concentrations as high as 25 nM[2].

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

    In Vivo

    The effect of Oleandrin is investigated on glioma growth in vivo. To this aim, SCID or C57BL/6 mice are transplanted, respectively, with human U87MG (5×104), U251, GBM19 (5×105), or murine (syngeneic) GL261 (7.5×104) cells into the right striatum and, after 10 d, treated daily with intraperitoneal Oleandrin for an additional 7 d. Oleandrin significantly reduces tumor sizes in human and murine glioma cell models in vivo in a dose-dependent way. High concentrations of Oleandrin (3 mg/kg) are fatal in both models, as expected from the known lethal dose for rodents. Doses of Oleandrin below the lethal dose (0.3 mg/kg) significantly increase the survival time from 32.6±1.4 d to 53.8±9.6 d in mice injected with U87MG cells (n=5-11; p<0.01, log-rank test) and from 23.37±1.2 d to 34.38±3.3 d (n=5-11; p<0.01, log rank test) in mice injected with GL261 cells[3].

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

    Clinical Trial
    Molecular Weight




    CAS No.



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    Structure Classification
    Initial Source

    Room temperature in continental US; may vary elsewhere.

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

    DMSO : 100 mg/mL (173.39 mM; Need ultrasonic)

    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.7339 mL 8.6697 mL 17.3394 mL
    5 mM 0.3468 mL 1.7339 mL 3.4679 mL
    10 mM 0.1734 mL 0.8670 mL 1.7339 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (4.33 mM); Clear solution

    • 2.

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

      Solubility: ≥ 2.5 mg/mL (4.33 mM); Clear solution

    • 3.

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

      Solubility: ≥ 2.5 mg/mL (4.33 mM); Clear solution

    *All of the co-solvents are available by MedChemExpress (MCE).
    Purity & Documentation

    Purity: 99.93%

    Cell Assay

    Undifferentiated wild-type and well-differentiated CaCO-2 cells are treated with a range of concentrations of Oleandrin (0.2-25 nM). After 48 h, cells are labeled with BrdU and relative cell proliferation is determined with a BrdU Cell Proliferation Kit[2].

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

    Animal Administration

    After tumor cell injection, SCID or C57BL/6 mice are monitored daily. The end point is determined by lack of physical activity or death. The mean survival time is calculated using the Kaplan-Meier method and statistical analysis is performed using a log-rank test. For cotreatment with Temozolomide (TMZ), 10 d after tumor injection, mice are treated with Oleandrin (0.03, 0.3, or 3 mg/kg/daily, i.p.), TMZ (50 mg/kg, i.p., every 2 d for a total of 4 times with a stop of 2 weeks) or both. The dosing scheme is chosen starting from these data to be reasonably sure that a constant concentration of drug is maintained along the experiment. Animals used in Kaplan-Meier survival studies receive up to four TMZ cycles.

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

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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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