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


Cat. No.: HY-13719 Purity: 99.84%
Handling Instructions

Oleandrin 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

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2 mg USD 216 In-stock
5 mg USD 336 In-stock
10 mg USD 576 In-stock
25 mg USD 1020 Get quote
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Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References


Oleandrin 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].

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].

Preparing Stock Solutions
Concentration Volume 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.
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.

Molecular Weight







O=C1OCC([[email protected]]2[[email protected]@H](OC(C)=O)C[[email protected]]3(O)[[email protected]]4([H])CC[[email protected]]5([H])C[[email protected]@H](O[[email protected]]6C[[email protected]@H]([[email protected]]([[email protected]](C)O6)O)OC)CC[[email protected]]5(C)[[email protected]@]4([H])CC[[email protected]]23C)=C1

Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month

Room temperature in continental US; may vary elsewhere

Solvent & Solubility


* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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