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

Bisoprolol hemifumarate  (Synonyms: 半富馬酸比索洛爾)

目錄號: HY-B0076 純度: 99.84%
COA 產(chǎn)品使用指南

Bisoprolol hemifumarate 是一種有效的、選擇性的、具有口服活性的 β1 腎上腺素受體 (β1-adrenergic receptor) 阻滯劑，對 β2 受體的活性很小。Bisoprolol hemifumarate 可用于高血壓，冠狀動脈疾病和穩(wěn)定的心室功能障礙的研究。

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Bisoprolol hemifumarate Chemical Structure

Bisoprolol hemifumarate Chemical Structure

CAS No. : 104344-23-2

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規(guī)格 價格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥231
In-stock
50 mg ￥210
In-stock
100 mg ￥360
In-stock
250 mg ￥720
In-stock
500 mg ￥1140
In-stock
1 g   詢價  
5 g   詢價  

* Please select Quantity before adding items.

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.

    查看 Adrenergic Receptor 亞型特異性產(chǎn)品:

    • 生物活性

    • 純度 & 產(chǎn)品資料

    • 參考文獻(xiàn)

    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

     

    體外研究
    (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).
    體內(nèi)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 號
    性狀

    固體

    顏色

    White to off-white

    中文名稱

    半富馬酸比索洛爾； 比索洛爾半富馬酸鹽
    運(yùn)輸條件

    Room temperature in continental US; may vary elsewhere.
    儲存方式

    4°C, sealed storage, away from moisture

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

    溶解性數(shù)據(jù)
    細(xì)胞實驗： 

    DMSO 中的溶解度 : ≥ 50 mg/mL (130.38 mM; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響，請使用新開封的 DMSO)

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

    * "≥" means soluble, but saturation unknown.

    配制儲備液
    濃度 溶劑體積 質(zhì)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
    查看完整儲備液配制表

    * 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
    儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C儲存時，請在6個月內(nèi)使用，-20°C儲存時，請在1個月內(nèi)使用。

    * 備注：如您選擇水作為儲備液，請稀釋至工作液后，再用 0.22 μm 的濾膜過濾除菌后使用。

    • 摩爾計算器

    • 稀釋計算器

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

    質(zhì)量
    =
    濃度
    ×
    體積
    ×
    分子量 *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    濃度 (start)

    C1

    ×
    體積 (start)

    V1

    =
    濃度 (final)

    C2

    ×
    體積 (final)

    V2

    動物實驗：

    以下溶解方案，請直接配制工作液。建議現(xiàn)用現(xiàn)配，在短期內(nèi)盡快用完。 以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比； 如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶。

    • 方案 一

      請依序添加每種溶劑： PBS

      Solubility: 100 mg/mL (260.77 mM); 澄清溶液; 超聲助溶

    動物溶解方案計算器
    請輸入動物實驗的基本信息：

    給藥劑量

    mg/kg

    動物的平均體重

    g

    每只動物的給藥體積

    μL

    動物數(shù)量

    只
    由于實驗過程有損耗，建議您多配一只動物的量
    計算結(jié)果
    工作液所需濃度 : mg/mL
    該產(chǎn)品水溶性佳，請具體參考實測 水 / PBS / Saline 中的溶解度數(shù)據(jù)。
    您所需的儲備液濃度超過該產(chǎn)品的實測溶解度，如有需要，請與 MCE 中國技術(shù)支持聯(lián)系。
    純度 & 產(chǎn)品資料
    參考文獻(xiàn)

    完整儲備液配制表

    * 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
    儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C儲存時，請在6個月內(nèi)使用，-20°C儲存時，請在1個月內(nèi)使用。

    可選溶劑 濃度 溶劑體積 質(zhì)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

    * 備注：如您選擇水作為儲備液，請稀釋至工作液后，再用 0.22 μm 的濾膜過濾除菌后使用。

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