Ouabain

产品描述

Ouabain是选择性Na+/K+-ATPase抑制剂,与α2 /α3亚基结合，Ki为41 nM/15 nM。

靶点

α2

α3

IC50

41 nM (Ki)

15 nM (Ki)

体外研究

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.

体内研究

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).

溶解性

DMSO 146 mg/mL，水<1 mg/mL，乙醇146 mg/mL

稳定性

2年-20°C粉状，6月-80°C溶于DMSO

特征

Ouabain is a glycoside poison that binds to and inhibits the action of the Na+/K+ pump in the cell membrane