Oleandrin

Additional information:
Oleandrin inhibits the Na+, K+-ATPase activity with an IC50 of 620 nM. Oleandrin induces apoptosis via activating endoplasmic reticulum stress.|Product information|CAS Number: 465-16-7|Molecular Weight: 576.72|Formula: C32H48O9|Chemical Name: (1R, 2S, 3aS, 3bR, 5aR, 7S, 9aS, 9bS, 11aR)-3a-hydroxy-7-{[(2R, 4S, 5S, 6S)-5-hydroxy-4-methoxy-6-methyloxan-2-yl]oxy}-9a, 11a-dimethyl-1-(5-oxo-2, 5-dihydrofuran-3-yl)-hexadecahydro-1H-cyclopenta[a]phenanthren-2-yl acetate|Smiles: CC(=O)O[C@H]1C[C@]2(O)[C@@H]3CC[C@@H]4C[C@H](CC[C@]4(C)[C@H]3CC[C@]2(C)[C@H]1C1COC(=O)C=1)O[C@H]1C[C@H](OC)[C@@H](O)[C@H](C)O1|InChiKey: JLPDBLFIVFSOCC-XYXFTTADSA-N|InChi: InChI=1S/C32H48O9/c1-17-29(35)24(37-5)14-27(39-17)41-21-8-10-30(3)20(13-21)6-7-23-22(30)9-11-31(4)28(19-12-26(34)38-16-19)25(40-18(2)33)15-32(23,31)36/h12,17,20-25,27-29,35-36H,6-11,13-16H2,1-5H3/t17-,20+,21-,22-,23+,24-,25-,27-,28-,29-,30-,31+,32-/m0/s1|Technical Data|Appearance: Solid Power|Purity: ≥98% (or refer to the Certificate of Analysis)|Solubility: Soluble in DMSO|Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.{{Abelacimab} medchemexpress|{Abelacimab} Metabolic Enzyme/Protease|{Abelacimab} Purity & Documentation|{Abelacimab} Description|{Abelacimab} manufacturer|{Abelacimab} Epigenetics} |Shelf Life: ≥360 days if stored properly.{{Darunavir} MedChemExpress|{Darunavir} Anti-infection|{Darunavir} Biological Activity|{Darunavir} In Vivo|{Darunavir} manufacturer|{Darunavir} Autophagy} |Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.PMID:33243080 |Drug Formulation: To be determined|HS Tariff Code: 382200|How to use|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. 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.|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; pReferences:|Jortani SA, et al. Inhibition of Na,K-ATPase by oleandrin and oleandrigenin, and their detection by digoxin immunoassays. Clin Chem. 1996 Oct;42(10):1654-8.Yang P, et al. Cellular location and expression of Na+, K+-ATPase α subunits affect the anti-proliferative activity of oleandrin. Mol Carcinog. 2014 Apr;53(4):253-63.Garofalo S, et al. The Glycoside Oleandrin Reduces Glioma Growth with Direct and Indirect Effects on Tumor Cells. J Neurosci. 2017 Apr 5;37(14):3926-3939.Products are for research use only. Not for human use.|