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编 号：F600587
分子式：C22H35NO8
分子量：441.52
分子式：C22H35NO8
分子量：441.52
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CAS No: 105878-43-1
产品详情
生物活性：
Bisoprolol fumarate is a potent, selective and orally active β1-adrenergic receptor blocker with little activity on β2-receptor. Bisoprolol fumarate has the potential for hypertension, coronary artery disease and stable ventricular dysfunction research.
体内研究：
Bisoprolol fumarate (oral administration, 5 mg/kg, for 1 week) increases left ventricular ejection fraction (LVEF) and decreases the heart rate value.Bisoprolol fumarate (oral gavage, 8 mg/kg, daily for four weeks) shows protective effects against Cadmium-induced myocardial toxicity in rats.Bisoprolol fumarate (oral gavage, 1 mg/kg, daily for 6 weeks) reversessmall conductance calcium-activated potassium channel (SK) remodeling in a volume-overload rat model.Animal Model:Ischemia/reperfusion (I/R) injury rats
Dosage:0.5, 5, 10 mg/kg
Administration:Oral administration, for 1 week, prior to 0.5 h ischemia/4 h reperfusion.
Result:Reduced infarct size from 44% in I/R group to 31% in treated group.
Animal Model:Cadmium-induced rats
Dosage:2, 8 mg/kg
Administration:Oral gavage, daily for four weeks.
Result:Decreased mean arterial pressure (MAP) at 8 mg/kg.Decreased serum biomarkers (ALT, AST) and NF-kB p65 expression and TNF-α levels (cardiac tissue samples) at 8 mg/kg.
体外研究：
Bisoprolol fumarate (2 μM, 1 h) protects myocardial cells (H9c2) from ischemia/reperfusion (I/R) injury.Bisoprolol fumarate (2 μM, 1 h) reduces the H/R-induced ROS production and apoptosis in H9c2 cells.Bisoprolol fumarate (2 μM, 1 h) increases AKT and GSK3β phosphorylation in H9c2 cells.Bisoprolol fumarate (100 μM, 24 h) reverses Epinephrine-inhibited emigration in cholesterol-loaded DCs (dendritic cell) through increasing in β-arrestin 2, CCR7 and PI3K phosphorylation.
Bisoprolol fumarate is a potent, selective and orally active β1-adrenergic receptor blocker with little activity on β2-receptor. Bisoprolol fumarate has the potential for hypertension, coronary artery disease and stable ventricular dysfunction research.
体内研究：
Bisoprolol fumarate (oral administration, 5 mg/kg, for 1 week) increases left ventricular ejection fraction (LVEF) and decreases the heart rate value.Bisoprolol fumarate (oral gavage, 8 mg/kg, daily for four weeks) shows protective effects against Cadmium-induced myocardial toxicity in rats.Bisoprolol fumarate (oral gavage, 1 mg/kg, daily for 6 weeks) reversessmall conductance calcium-activated potassium channel (SK) remodeling in a volume-overload rat model.Animal Model:Ischemia/reperfusion (I/R) injury rats
Dosage:0.5, 5, 10 mg/kg
Administration:Oral administration, for 1 week, prior to 0.5 h ischemia/4 h reperfusion.
Result:Reduced infarct size from 44% in I/R group to 31% in treated group.
Animal Model:Cadmium-induced rats
Dosage:2, 8 mg/kg
Administration:Oral gavage, daily for four weeks.
Result:Decreased mean arterial pressure (MAP) at 8 mg/kg.Decreased serum biomarkers (ALT, AST) and NF-kB p65 expression and TNF-α levels (cardiac tissue samples) at 8 mg/kg.
体外研究：
Bisoprolol fumarate (2 μM, 1 h) protects myocardial cells (H9c2) from ischemia/reperfusion (I/R) injury.Bisoprolol fumarate (2 μM, 1 h) reduces the H/R-induced ROS production and apoptosis in H9c2 cells.Bisoprolol fumarate (2 μM, 1 h) increases AKT and GSK3β phosphorylation in H9c2 cells.Bisoprolol fumarate (100 μM, 24 h) reverses Epinephrine-inhibited emigration in cholesterol-loaded DCs (dendritic cell) through increasing in β-arrestin 2, CCR7 and PI3K phosphorylation.
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