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Ouabain Octahydrate(Acocantherine)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Ouabain Octahydrate(Acocantherine)图片
CAS NO:11018-89-6
规格:≥98%
包装与价格:
包装价格(元)
50mg电议
100mg电议
250mg电议
500mg电议
1g电议
10g电议

产品介绍
理化性质和储存条件
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 infoChemical 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([C@H]2CC[C@]3(O)[C@]4([H])CCC5(O)CC(O[C@H]6[C@@H]([C@@H]([C@H]([C@H](C)O6)O)O)O)CC(O)[C@]5(CO)[C@@]4([H])[C@H](O)C[C@]23C)=C1
SynonymsNSC 25485; Acocantherin; G-Strophanthin; Strodival; NSC-25485; NSC25485
实验参考方法
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.