product name Ouabain Octahydrate
Description: Ouabain is a potent and selective Na+/K+, -ATPase inhibitor, binds to α2 /α3 subunit with Ki of 41 nM/15 nM. 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 are confined to a reticular distribution within the PM that paralleled underlying endoplasmic or sarcoplasmic reticulum.
References: J Biol Chem. 1991 May 15;266(14):9327-31; Proc Natl Acad Sci U S A. 1997 Mar 4;94(5):1800-5.
728.77
Formula
C29H44O12.8H2O
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)
Solubility (In vivo)
Synonyms
NSC 25485
other peoduct :
| 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: |
|---|---|
| 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). |
| Animal model | Male Wistar rats with heart failure due to myocardial infarction (MI) |
| Formulation & Dosage | Dissolved in saline; 14.4 mg/kg; s.c. injection |
| References | J 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. |
