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

Oleandrin 

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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10 mM * 1 mL in DMSO USD 426 In-stock
Estimated Time of Arrival: December 31
2 mg USD 216 In-stock
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5 mg USD 336 In-stock
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10 mg USD 576 In-stock
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25 mg USD 1020 In-stock
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Description

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].

Molecular Weight

576.72

Formula

C₃₂H₄₈O₉

CAS No.

465-16-7

SMILES
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
References
Cell Assay
[2]

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
[3]

Mice[3]
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.

References

Purity: 99.84%

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Oleandrin
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