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

Bisoprolol hemifumarate  (Synonyms: 半富马酸比索洛尔)

目录号: HY-B0076 纯度: 99.73%
COA 产品使用指南

Bisoprolol hemifumarate 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 hemifumarate 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。

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Bisoprolol hemifumarate Chemical Structure

Bisoprolol hemifumarate Chemical Structure

CAS No. : 104344-23-2

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥231
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50 mg ¥210
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100 mg ¥360
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250 mg ¥720
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500 mg ¥1140
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Other Forms of Bisoprolol hemifumarate:

    Bisoprolol hemifumarate 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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    • 生物活性

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Bisoprolol hemifumarate is a potent, selective and orally active β1-adrenergic receptor blocker with little activity on β2-receptor. Bisoprolol hemifumarate 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 hemifumarate (2 μM, 1 h) protects myocardial cells (H9c2) from ischemia/reperfusion (I/R) injury[2].
    Bisoprolol hemifumarate (2 μM, 1 h) reduces the H/R-induced ROS production and apoptosis in H9c2 cells[2].
    Bisoprolol hemifumarate (2 μM, 1 h) increases AKT and GSK3β phosphorylation in H9c2 cells[2].
    Bisoprolol hemifumarate (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).
    体内研究
    (In Vivo)

    Bisoprolol hemifumarate (oral administration, 5 mg/kg, for 1 week) increases left ventricular ejection fraction (LVEF) and decreases the heart rate value[2].
    Bisoprolol hemifumarate (oral gavage, 8 mg/kg, daily for four weeks) shows protective effects against Cadmium-induced myocardial toxicity in rats[4].
    Bisoprolol hemifumarate (oral gavage, 1 mg/kg, daily for 6 weeks) reversessmall 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
    分子量

    383.48

    Formula

    C18H31NO4.1/2C4H4O4

    CAS 号
    性状

    固体

    颜色

    White to off-white

    中文名称

    半富马酸比索洛尔; 比索洛尔半富马酸盐

    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    溶解性数据
    细胞实验: 

    DMSO 中的溶解度 : ≥ 50 mg/mL (130.38 mM; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

    H2O 中的溶解度 : 20 mg/mL (52.15 mM; 超声助溶)

    * "≥" means soluble, but saturation unknown.

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 2.6077 mL 13.0385 mL 26.0770 mL
    5 mM 0.5215 mL 2.6077 mL 5.2154 mL
    查看完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
    储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

    * 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

    • 摩尔计算器

    • 稀释计算器

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    质量
    =
    浓度
    ×
    体积
    ×
    分子量 *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start)

    C1

    ×
    体积 (start)

    V1

    =
    浓度 (final)

    C2

    ×
    体积 (final)

    V2

    动物实验:

    以下溶解方案,请直接配制工作液。建议现用现配,在短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比; 如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶。

    • 方案 一

      请依序添加每种溶剂: PBS

      Solubility: 100 mg/mL (260.77 mM); 澄清溶液; 超声助溶

    动物溶解方案计算器
    请输入动物实验的基本信息:

    给药剂量

    mg/kg

    动物的平均体重

    g

    每只动物的给药体积

    μL

    动物数量

    由于实验过程有损耗,建议您多配一只动物的量
    计算结果
    工作液所需浓度 : mg/mL
    该产品水溶性佳,请具体参考实测 水 / PBS / Saline 中的溶解度数据。
    您所需的储备液浓度超过该产品的实测溶解度,如有需要,请与 MCE 中国技术支持联系。
    纯度 & 产品资料
    参考文献

    完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
    储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    H2O / DMSO 1 mM 2.6077 mL 13.0385 mL 26.0770 mL 65.1924 mL
    5 mM 0.5215 mL 2.6077 mL 5.2154 mL 13.0385 mL
    10 mM 0.2608 mL 1.3038 mL 2.6077 mL 6.5192 mL
    15 mM 0.1738 mL 0.8692 mL 1.7385 mL 4.3462 mL
    20 mM 0.1304 mL 0.6519 mL 1.3038 mL 3.2596 mL
    25 mM 0.1043 mL 0.5215 mL 1.0431 mL 2.6077 mL
    30 mM 0.0869 mL 0.4346 mL 0.8692 mL 2.1731 mL
    40 mM 0.0652 mL 0.3260 mL 0.6519 mL 1.6298 mL
    50 mM 0.0522 mL 0.2608 mL 0.5215 mL 1.3038 mL
    DMSO 60 mM 0.0435 mL 0.2173 mL 0.4346 mL 1.0865 mL
    80 mM 0.0326 mL 0.1630 mL 0.3260 mL 0.8149 mL
    100 mM 0.0261 mL 0.1304 mL 0.2608 mL 0.6519 mL

    * 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

    Help & FAQs
    • 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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