Ouabain

製品コードS4016 バッチS401607

印刷

化学情報

Chemical Structure Synonyms NSC 25485 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C29H44O12.8H2O
分子量 728.77 CAS No. 630-60-4
Solubility (25°C)* 体外 DMSO 100 mg/mL (137.21 mM)
Water Insoluble
Ethanol Insoluble
* <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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 Ouabain (NSC 25485) is a selective Na+/K+, -ATPase inhibitor, binds to α2 /α3 subunit with Ki of 41 nM/15 nM.This product is a hazardous chemical (acute toxicity/flammable/skin corrosive). Please use it while wearing a protective face mask, gloves, and clothing.
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]
特徴 A glycoside poison that binds to and inhibits the action of the Na+/K+ pump in the cell membrane.

プロトコル(参考用のみ)

キナーゼアッセイ 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.
動物実験 動物モデル Male Wistar rats with heart failure due to myocardial infarction (MI)
投薬量 14.4 mg/kg
投与方法 Subcutaneous

カスタマーフィードバック

Data from [Data independently produced by , , Antiviral Res, 2016, 132:38-45.]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

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Cell surface thermal proteome profiling tracks perturbations and drug targets on the plasma membrane [ Nat Methods, 2021, 18(1):84-91] PubMed: 33398190
Genome-scale CRISPR screening identifies cell cycle and protein ubiquitination processes as druggable targets for erlotinib-resistant lung cancer [ Mol Oncol, 2020, 10.1002/1878-0261.12853] PubMed: 33188726
Genome-scale CRISPR screening identifies cell cycle and protein ubiquitination processes as druggable targets for erlotinib-resistant lung cancer [ Mol Oncol, 2020, 10.1002/1878-0261.12853] PubMed: 33188726
Reversal of Infected Host Gene Expression Identifies Repurposed Drug Candidates for COVID-19 [ bioRxiv, 2020, 2020/9/20.4.7.30734] PubMed: 32511305
Temporal Metabolite, Ion, and Enzyme Activity Profiling Using Fluorescence Microscopy and Genetically Encoded Biosensors. [ Methods Mol Biol, 2019, 1978:343-353] PubMed: 31119673
Cyclopiazonic acid, an inhibitor of calcium-dependent ATPases with antiviral activity against human respiratory syncytial virus [Cui R, et al. Antiviral Res, 2016, 132:38-45] PubMed: 27210812
Thermal proteome profiling monitors ligand interactions with cellular membrane proteins [Reinhard FB Nat Methods, 2015, 12(12):1129-31] PubMed: 26524241

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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