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。

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 [1] [2].

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).

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.

105878-43-1

C22H35NO8

441.521

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years