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Bisoprolol fumarate
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。
Bisoprolol fumarate图片
CAS NO:105878-43-1
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品名称
比索洛尔富马酸盐
产品介绍
Bisoprolol fumarate 是一种有效的、选择性的、具有口服活性的 β1 肾上腺素受体 (β1-adrenergic receptor) 阻滞剂,对 β2 受体的活性很小。Bisoprolol fumarate 可用于高血压,冠状动脉疾病和稳定的心室功能障碍的研究。
生物活性

Bisoprolol fumarate is a potent, selective and orally activeβ1-adrenergic receptorblocker with little activity on β2-receptor. Bisoprolol fumarate has the potential for hypertension, coronary artery disease and stable ventricular dysfunction research[1][2].

IC50& Target[1]

Beta-1 adrenergic receptor

 

体外研究
(In Vitro)

Bisoprolol fumarate (2 μM, 1 h) protects myocardial cells (H9c2) from ischemia/reperfusion (I/R) injury[2].
Bisoprolol fumarate (2 μM, 1 h) reduces the H/R-induced ROS production and apoptosis in H9c2 cells[2].
Bisoprolol fumarate (2 μM, 1 h) increases AKT and GSK3β phosphorylation in H9c2 cells[2].
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[3].

Cell Viability Assay[2]

Cell Line:H9c2 cells
Concentration:0.2, 2, 20 μM
Incubation Time:1 h
Result:Elevated the survival rates of cardiomyocytes subjected to H/R (hypoxia/reoxygenation) to 73.20%, 90.38%, 81.25% respectively.

Cell Migration Assay[3]

Cell Line:DCs
Concentration:100 μM
Incubation Time:6, 12, 24 h
Result:Increased the amount of migrating cells by 46.00% (6 h), 64.25% (12 h) and 55.74% (24 h).
体内研究
(In Vivo)

Bisoprolol fumarate (oral administration, 5 mg/kg, for 1 week) increases left ventricular ejection fraction (LVEF) and decreases the heart rate value[2].
Bisoprolol fumarate (oral gavage, 8 mg/kg, daily for four weeks) shows protective effects against Cadmium-induced myocardial toxicity in rats[4].
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[5].

Animal Model:Ischemia/reperfusion (I/R) injury rats[2]
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[4]
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.
Clinical Trial
分子量

441.52

Formula

C22H35NO8

CAS 号

105878-43-1

中文名称

比索洛尔富马酸盐

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.