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    Ouabain Octahydrate (Acocantherine)
    Ouabain Octahydrate (Acocantherine)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V1665
    CAS #: 11018-89-6Purity ≥98%

    Description: Ouabain (Ouabain Octahydrate; Acocantherine; G-Strophanthin) is a novel, potent and selective Na+/K+, -ATPase inhibitor, which binds to α2 /α3 subunit with Ki of 41 nM/15 nM. Ouabain (100 nM) inhibits ATPase activities with 25%. Ouabain (0.1 μM-1.0 μM) inhibits the Na+ pump and increases stored Ca2+ in cultured rat astrocytes. High Ouabain affinity isoforms are confined to a reticular distribution within the PM that paralleled underlying endoplasmic or sarcoplasmic reticulum.

    References: J Biol Chem. 1991 May 15;266(14):9327-31; Proc Natl Acad Sci U S A. 1997 Mar 4;94(5):1800-5.


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    Molecular Weight (MW)728.77 
    FormulaC29H44O12.8H2O 
    CAS No.11018-89-6
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 100 mg/mL (137.2 mM)
    Water: <1 mg/mL
    Ethanol: 100 mg/mL (137.2 mM)
    Other infoIUPAC/Chemical Name: 3-(6-Deoxy-alpha-L-mannopyranosyloxy)-1,5,11a,14,19-pentahydroxycard-20(22)-enolide
    InChi Key: LPMXVESGRSUGHW-KAPJGFEOSA-N
    InChi Code: InChI=1S/C29H44O12/c1-13-22(34)23(35)24(36)25(40-13)41-15-8-19(32)28(12-30)21-17(3-5-27(28,37)9-15)29(38)6-4-16(14-7-20(33)39-11-14)26(29,2)10-18(21)31/h7,13,15-19,21-25,30-32,34-38H,3-6,8-12H2,1-2H3/t13-,15?,16+,17+,18+,19?,21+,22-,23+,24+,25-,26+,27?,28+,29-/m0/s1
    SMILES Code: O=C1OCC([[email protected]]2CC[[email protected]]3(O)[[email protected]]4([H])CCC5(O)CC(O[[email protected]]6[[email protected]@H]([[email protected]@H]([[email protected]]([[email protected]](C)O6)O)O)O)CC(O)[[email protected]]5(CO)[[email protected]@]4([H])[[email protected]](O)C[[email protected]]23C)=C1
    SynonymsNSC 25485; Acocantherin; G-Strophanthin; Strodival; NSC-25485; NSC25485


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    In Vitro

    In vitro activity: Ouabain (100 nM) inhibits ATPase activities with 25%. Ouabain (0.1 μM-1.0 μM) inhibits the Na+ pump and increases stored Ca2+ in cultured rat astrocytes. High Ouabain affinity isoforms (alpha2 in astrocytes, alpha3 in neurons and myocytes) are confined to a reticular distribution within the PM that paralleled underlying endoplasmic or sarcoplasmic reticulum. Ouabain (0.5-1.0 mM) increases the levels of alpha1 and beta1 mRNAs, whereas it decreases those of alpha2 and beta2 mRNAs in cultured rat astrocytes. Ouabain increases alpha1 and beta1, but not alpha2 and beta2, proteins, and that the isoforms in control and ouabain-treated cultures. The ouabain-induced increase in alpha1 mRNA is blocked by cycloheximide (10 mM), the intracellular Ca2+ chelator 1,2-bis(2-aminophenoxy)ethane-N,N,N',N'-tetraacetic acid tetraacetoxymethyl ester (30 mM), and FK506 (1 nM) in cultured rat astrocytes. Ouabain (10 μM) induces significant PMD in both cell lines (28.1% of MDCK cells and 47.9% of Ma104 cells are gated in region M1, against 11.8% and 14.6% of the respective controls), but unexpectedly this effect is more remarkable in Ma104 cells. Ouabain (10 μM) induces a sustained increase in P-Tyr in MDCK cells and GSH almost completely reverted this effect, while the effect is not significant in Ma104 cells.


    Kinase Assay: Ouabain Octahydrate is a Na(+)/K(+) ATPase inhibitor. Ouabain (100 nM) inhibits ATPase activities with 25%. Ouabain (0.1 μM-1.0 μM) inhibits the Na+ pump and increases stored Ca2+ in cultured rat astrocytes. High Ouabain affinity isoforms (alpha2 in astrocytes, alpha3 in neurons and myocytes) are confined to a reticular distribution within the PM that paralleled underlying endoplasmic or sarcoplasmic reticulum. Ouabain (0.5-1.0 mM) increases the levels of alpha1 and beta1 mRNAs, whereas it decreases those of alpha2 and beta2 mRNAs in cultured rat astrocytes. Ouabain increases alpha1 and beta1, but not alpha2 and beta2, proteins, and that the isoforms in control and ouabain-treated cultures. The ouabain-induced increase in alpha1 mRNA is blocked by cycloheximide (10 mM), the intracellular Ca2+ chelator 1,2-bis(2-aminophenoxy)ethane-N,N,N',N'-tetraacetic acid tetraacetoxymethyl ester (30 mM), and FK506 (1 nM) in cultured rat astrocytes.


    Cell Assay: Cell viability is determined using a Cell Counting Kit-8 assay. Briefly, 100 μL Raji cells (5×104/mL) are seeded in triplicate in a 96-well plate and treated with various concentrations of ouabain (400, 200, 100, 50, 25, 12.5, 6.25, 3.13, 1.56, 0.78 and 0.39 nM) for 48 h. Following the 48-h treatment, 10 μL CCK-8 reagent is added to each well, and the cells are incubated for an additional 3 h at 37°C. Optical density (OD) values at 450 nm are subsequently measured, and each ouabain concentration is assessed in triplicate. Raji cells cultured in medium without drug served as controls. Cell viability is calculated according to the following formula: Inhibition rate (%)=[1 − (OD450(sample) − OD450(blank))/(OD450(control) − OD450(blank))] × 100.

    In VivoOuabain (14.4 mg/kg.d s.c. intermittent) further increases total peripheral resistance (TPR) in rats with heart failure due to myocardial infarction (MI), while continuous Ouabain treatment normalized TPR in rats. Ouabain (14.4 mg/kg.d s.c. continuous) significantly improves basal and maximal CO (basal: 83 mL/min; maximal: 134 mL/min).  
    Animal modelMale Wistar rats with heart failure due to myocardial infarction (MI) 
    Formulation & DosageDissolved in saline; 14.4 mg/kg; s.c. injection 
    ReferencesJ Biol Chem. 1991 May 15;266(14):9327-31; Proc Natl Acad Sci U S A. 1997 Mar 4;94(5):1800-5; Naunyn Schmiedebergs Arch Pharmacol. 1997 Aug;356(2):203-9. 


    These protocols are for reference only. InvivoChem does not independently validate these methods.

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