物质信息

ID:73658

名称和标识
别名
Sodium orthovanadate
IUPAC传统名
3-oxo-3-(sodiooxy)-2,4-dioxa-3-vanada-1,5-disodapentane
IUPAC标准名
3-oxo-3-(sodiooxy)-2,4-dioxa-3-vanada-1,5-disodapentane
数据登录号
化合物性质
安全信息
保存条件
-20°C
产品相关信息
成盐信息
Sodium Salt
描述信息
Research Area
Description
Cancer
Biological Activity
Description
Sodium orthovanadate is an alkaline phosphatase and (Na,K)-ATPase inhibitor with IC50 of 10 μM.
Targets
Phosphatase
IC50
10 μM [1]
In Vitro
In transient forebrain ischemia, Sodium orthovanadate rescues cells from delayed neuronal death in the hippocampal CA1 region. The neuroprotective effects of Sodium orthovanadate and IGF-1 are associated with preventing decreased Akt-Ser-473 phosphorylation in the CA1 region observed immediately after reperfusion. Akt is moderately activated in the cell bodies and dendrites of pyramidal neurons after orthovanadate treatment. The Sodium orthovanadate treatment also prevents the decrease in phosphorylation of mitogen-activated protein kinase (MAPK). [3] Sodium orthovanadate inhibits ASK1 through the PI3-K/Akt-dependent pathway. [4] Sodium orthovanadate up-regulates Akt activity in the brain and in turn rescue neurons from delayed neuronal death by inhibiting FKHR-dependent or -independent death signals in neurons. [4]
In Vivo
In a rat model of myocardial ischemic infarction, sodium orthovanadate rescues cells from ischemia/reperfusion injuries. Post-treatment with Sodium orthovanadate reduces infarct size in a dose-dependent manner. [5] Sodium orthovanadate treatment also ameliorates contractile dysfunction of the left ventricle 72 hours after reperfusion. The cytoprotective action of Sodium orthovanadate treatment is closely associated with inhibition of fodrin breakdown. Sodium orthovanadate treatment inhibits caspase-3 activation induced by ischemia. [6]
Clinical Trials
Features
Protocol
Kinase Assay [2]
ATPase assay
The coupled assay linking ADP production to NADH oxidation is used for all ATPase assays. The fraction of active enzyme is determined by measuring enzyme activity after linearity has been achieved by the activity prior to addition of Sodium orthovanadate. Final steady state hydrolysis rates are independent of the order addition of Sodium orthovanadate and enzyme.
Cell Assay []
Animal Study [6]
Animal Models
Male Sprague-Dawley rats
Formulation
0.9% saline
Doses
0.005 mL/min/100g of b.wt. over 20 minutes
Administration
Administered via i.v.
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参考文献
• Cantley LC Jr, et al. J Biol Chem, 1977, 252(21), 7421-7423.
• Wu DN, et al. Neurosci Lett, 2006, 404(1-2), 98-102.
• Kawano T, et al. J Cereb Blood Flow Metab, 2001, 21(11), 1268-1280.
• Takada Y, et al. J Pharmacol Exp Ther, 2004, 311(3), 1249-1255.
• Fukunaga K, et al. J Pharmacol Sci, 2005, 98(3), 205-211.
• Wu Y, et al. Acta Pharmacol Sin, 2005, 26(3), 345-352.
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