Ouabain

Catalog No.S4016

Ouabain is a selective Na+/K+, -ATPase inhibitor, binds to α2 /α3 subunit with Ki of 41 nM/15 nM.

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In DMSO USD 220 In stock
USD 170 In stock
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Ouabain Chemical Structure

Ouabain Chemical Structure
Molecular Weight: 728.77

Validation & Quality Control

Quality Control & MSDS

Product Information

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Product Description

Biological Activity

Description Ouabain is a selective Na+/K+, -ATPase inhibitor, binds to α2 /α3 subunit with Ki of 41 nM/15 nM.
Targets α2 α3
IC50 41 nM (Ki) 15 nM (Ki) [1]
In vitro Ouabain (100 nM) inhibits ATPase activities with 25%. [1] 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. [2] 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. [3] 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. [4]
In vivo Ouabain (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). [5]
Features A glycoside poison that binds to and inhibits the action of the Na+/K+ pump in the cell membrane.

Protocol(Only for Reference)

Kinase Assay: [1]

Binding assays All binding assays are carried out with 50-100 μg of membrane protein in 1 mL aliquots containing 50 mM Tris maleate, pH 7.2, 5 mM MgCl2, 0.1 mM sodium ortho-vanadate, and different concentrations of ouabain (0.1 nM to 1 μM, specific activity ranging from 15.4 Ci/mmol to 0.12 Ci/mmol) for 2 hour at 37℃. Binding is terminated by dilution with 4 mL of ice-cold wash buffer (5 mM MgCl2, 5 mM Tris phosphate, and 50 mM Tris maleate, pH 7.4) and filtration through Whatman GF/F filters that are presoaked in 0.1% bovine serum albumin. The filters are washed four times for 2s each with 4 mL of wash buffer. Nonspecific binding, defined as the residual radioactivity seen in the presence of 2 mM unlabeled ouabain, accounted for 5-15% of total binding.

Animal Study: [5]

Animal Models Male Wistar rats with heart failure due to myocardial infarction (MI)
Dosages 14.4 mg/kg
Administration Subcutaneous
Solubility 0.5% methylcellulose/0.2% Tween 80 5 mg/mL
1

References

Clinical Trial Information( data from http://clinicaltrials.gov)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT00800228 Completed Hypertension National Institute on Aging (NIA) 2003-03
NCT00415038 Completed Essential Hypertension sigma-tau i.f.r. S.p.A. 2005-02 Phase 2
NCT01128101 Recruiting Renal Failure UPECLIN HC FM Botucatu Unesp 2011-03 Phase 4

Chemical Information

Download Ouabain SDF
Molecular Weight (MW) 728.77
Formula

C29H44O12.8H2O

CAS No. 630-60-4
Storage 3 years -20℃Powder
6 months-80℃in DMSO
Syonnyms N/A
Solubility (25°C) * In vitro DMSO 146 mg/mL (200 mM)
Water <1 mg/mL (<1 mM)
Ethanol 146 mg/mL (200 mM)
In vivo 0.5% methylcellulose/0.2% Tween 80 5 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name Card-20(22)-enolide, 3-[(6-deoxy-α-L-mannopyranosyl)oxy]-1,5,11,14,19-pentahydroxy-, hydrate (1:8), (1β,3β,5β,11α)-

Preparing Stock Solutions

Stock Solution (1ml DMSO) 1mM 10mM 20mM 30mM
Mass(mg) 0.72877 7.2877 14.5754 21.8631

Research Area

Tech Support & FAQs

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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