1. GPCR/G Protein Neuronal Signaling
  2. Adrenergic Receptor
  3. Bisoprolol

Bisoprolol  (Synonyms: 比索洛尔)

目录号: HY-129029

Bisoprolol 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 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。

在相同的摩尔浓度下,化合物盐形式与游离形式有相同的生物活性,但盐形式 Bisoprolol hemifumarate 通常具有更好的水溶性和稳定性。

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Bisoprolol Chemical Structure

Bisoprolol Chemical Structure

CAS No. : 66722-44-9

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Top Publications Citing Use of Products

    Bisoprolol purchased from MCE. Usage Cited in: Mol Neurobiol. 2019 Jan;56(1):367-377.  [Abstract]

    Inhibitory effect of bisoprolol fumarate on PrPSc accumulation in N2a-FK cells. After the cells are incubated in medium mixed with each concentration of sample compound or water (negative control) for 48 h, the collected cell lysates are digested with proteinase K. Western blotting is then performed for quantification of the PrPSc level.

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    • 参考文献


    Bisoprolol is a potent, selective and orally active β1-adrenergic receptor blocker with little activity on β2-receptor. Bisoprolol has the potential for hypertension, coronary artery disease and stable ventricular dysfunction research[1][2].

    IC50 & Target[1]

    Beta-1 adrenergic receptor


    (In Vitro)

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

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    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).
    (In Vivo)

    Bisoprolol (oral administration, 5 mg/kg, for 1 week) increases left ventricular ejection fraction (LVEF) and decreases the heart rate value[2].
    Bisoprolol (oral gavage, 8 mg/kg, daily for four weeks) shows protective effects against Cadmium-induced myocardial toxicity in rats[4].
    Bisoprolol (oral gavage, 1 mg/kg, daily for 6 weeks) reverses small conductance calcium-activated potassium channel (SK) remodeling in a volume-overload rat model[5].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    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




    CAS 号



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    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.


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