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Ouabain Octahydrate

Catalog No.GC10579

Ouabain Octahydrate is a Na+/K+-ATPase inhibitor that can be used to study congestive heart failure.

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Ouabain Octahydrate Chemical Structure

Cas No.: 11018-89-6

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10mM (in 1mL DMSO)
$39.00
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50mg
$39.00
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100mg
$67.00
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500mg
$200.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Description of Ouabain Octahydrate

Ouabain Octahydrate is a Na+/K+-ATPase inhibitor that can be used to study congestive heart failure[1]. Ouabain Octahydrate can be used to induce cardiac dysfunction or hypertension models in animal models[2]. Ouabain Octahydrate can exert anti-cancer activity by downregulating intracellular signal transducer and activator of transcription 3 (STAT3)[3].

In vitro, Ouabain Octahydrate (3nM) treatment of autosomal dominant polycystic kidney disease (ADPKD) cells for 24h reduced the expression of epithelial cell marker E-cadherin in ADPKD cells, and increased the expression of mesenchymal cell markers N-cadherin, α-smooth muscle actin (αSMA), type I collagen, and tight junction proteins occludin and claudin-1[4]. Ouabain Octahydrate (25, 50, 100nM) treated Burkitt lymphoma Raji cells for 48h inhibited cell proliferation in a dose-dependent manner, significantly reduced cell viability, and induced cell autophagy[5].

In vivo, Ouabain Octahydrate (3mg/kg) was intraperitoneally injected into LPS-pretreated WT, IL-1β−/−, NLRP3−/−, Casp1−/− mice, which significantly reduced left ventricular systolic function in WT mice, increased plasma CPK levels and cardiac IL-1β protein levels, induced macrophage infiltration and myocardial damage, but these effects were significantly attenuated in IL-1β⁻/⁻, NLRP3⁻/⁻, and Casp1⁻/⁻ mice[6].

References:
[1] Harich O O, Gavriliuc O I, Ordodi V L, et al. In Vitro Study of the Multimodal Effect of Na+/K+ ATPase Blocker Ouabain on the Tumor Microenvironment and Malignant Cells[J]. Biomedicines, 2023, 11(8): 2205.
[2] Ferrari P, Ferrandi M, Valentini G, et al. Targeting Ouabain-and Adducin-dependent mechanisms of hypertension and cardiovascular remodeling as a novel pharmacological approach[J]. Medical Hypotheses, 2007, 68(6): 1307-1314.
[3] Du J, Jiang L, Chen F, et al. Cardiac glycoside ouabain exerts anticancer activity via downregulation of STAT3[J]. Frontiers in oncology, 2021, 11: 684316.
[4] Venugopal J, McDermott J, Sanchez G, et al. Ouabain promotes partial epithelial to mesenchymal transition (EMT) changes in human autosomal dominant polycystic kidney disease (ADPKD) cells[J]. Experimental cell research, 2017, 355(2): 142-152.
[5] Meng L, Wen Y, Zhou M, et al. Ouabain induces apoptosis and autophagy in Burkitt’s lymphoma Raji cells[J]. Biomedicine & Pharmacotherapy, 2016, 84: 1841-1848.
[6] Kobayashi M, Usui-Kawanishi F, Karasawa T, et al. The cardiac glycoside ouabain activates NLRP3 inflammasomes and promotes cardiac inflammation and dysfunction[J]. PloS one, 2017, 12(5): e0176676.

Protocol of Ouabain Octahydrate

Cell experiment [1]:

Cell lines

Autosomal dominant polycystic kidney disease (ADPKD) cells、normal human kidney (NHK) cells

Preparation Method

Cultured ADPKD and NHK cells were treated without and with 3nM Ouabain Octahydrate for 24h. Cells were lysed and proteins of interest were identified by immunoblot.

Reaction Conditions

3nM; 24h

Applications

ADPKD cells respond to Ouabain Octahydrate with a decrease in expression of the epithelial marker E-cadherin and increase in the expression of the mesenchymal markers N-cadherin, α smooth muscle actin (αSMA) and collagen-I, and the tight junction protein occludin and claudin-1. Other adhesion molecules, such as ZO-1, β-catenin and vinculin were not significantly modified by Ouabain Octahydrate.These effects of Ouabain Octahydrate were not observed in normal human kidney (NHK) cells.

Animal experiment [2]:

Animal models

WT, IL-1β−/−, NLRP3−/−, Casp1−/− mice

Preparation Method

Mice were "primed" by intraperitoneal injection of low-dose lipopolysaccharide (LPS, 2mg/kg). 12h after LPS injection, Ouabain Octahydrate (3mg/kg) was injected intraperitoneally; the control group was injected with an equal volume of normal saline. Left ventricular systolic function (%FS, EF), left ventricular end-diastolic diameter (LVEDD) and end-systolic diameter (LVESD) were evaluated by echocardiography. Plasma creatine phosphokinase (CPK, a marker of myocardial injury) and cardiac tissue IL-1β levels were detected by ELISA.

Dosage form

3mg/kg; i.p.

Applications

Ouabain Octahydrate (3mg/kg) significantly reduced left ventricular systolic function (decreased %FS and EF, increased LVESD), increased plasma CPK levels and cardiac IL-1β protein levels only in LPS-pretreated WT mice. These effects were significantly attenuated in IL-1β⁻/⁻, NLRP3⁻/⁻, or Casp1⁻/⁻  mice.

References:
[1] Venugopal J, McDermott J, Sanchez G, et al. Ouabain promotes partial epithelial to mesenchymal transition (EMT) changes in human autosomal dominant polycystic kidney disease (ADPKD) cells[J]. Experimental cell research, 2017, 355(2): 142-152.
[2]Kobayashi M, Usui-Kawanishi F, Karasawa T, et al. The cardiac glycoside ouabain activates NLRP3 inflammasomes and promotes cardiac inflammation and dysfunction[J]. PloS one, 2017, 12(5): e0176676.

Chemical Properties of Ouabain Octahydrate

Cas No. 11018-89-6 SDF
Chemical Name 3-[(1R,3S,5S,8R,9S,10R,11R,13R,14S,17R)-1,5,11,14-tetrahydroxy-10-(hydroxymethyl)-13-methyl-3-[(2R,3R,4R,5R,6S)-3,4,5-trihydroxy-6-methyloxan-2-yl]oxy-2,3,4,6,7,8,9,11,12,15,16,17-dodecahydro-1H-cyclopenta[a]phenanthren-17-yl]-2H-furan-5-one
Canonical SMILES CC1C(C(C(C(O1)OC2CC(C3(C4C(CCC3(C2)O)C5(CCC(C5(CC4O)C)C6=CC(=O)OC6)O)CO)O)O)O)O
Formula C29H60O20 M.Wt 728.77
Solubility ≥ 19.5mg/mL in H20 with ultrasonic and warming Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of Ouabain Octahydrate

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1 mg 5 mg 10 mg
1 mM 1.3722 mL 6.8609 mL 13.7218 mL
5 mM 0.2744 mL 1.3722 mL 2.7444 mL
10 mM 0.1372 mL 0.6861 mL 1.3722 mL
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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3. All of the above co-solvents are available for purchase on the GlpBio website.

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Average Rating: 5 ★★★★★ (Based on Reviews and 28 reference(s) in Google Scholar.)

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