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

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.

For research use only. We do not sell to patients.

Bisoprolol hemifumarate Chemical Structure

Bisoprolol hemifumarate Chemical Structure

CAS No. : 104344-23-2

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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
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10 mM * 1 mL in DMSO USD 39 In-stock
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100 mg USD 60 In-stock
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Customer Review

Based on 6 publication(s) in Google Scholar

Other Forms of Bisoprolol hemifumarate:

Top Publications Citing Use of Products

    Bisoprolol hemifumarate purchased from MedChemExpress. 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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    Description

    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

     

    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].

    MedChemExpress (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 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].

    MedChemExpress (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
    Molecular Weight

    383.48

    Formula

    C18H31NO4.1/2C4H4O4

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    OC(CNC(C)C)COC1=CC=C(COCCOC(C)C)C=C1.OC(/C=C/C(O)=O)=O.[1/2]

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    4°C, sealed storage, away from moisture

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

    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 50 mg/mL (130.38 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : 20 mg/mL (52.15 mM; Need ultrasonic)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 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
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

    • Molarity Calculator

    • Dilution Calculator

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

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    In Vivo:

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  PBS

      Solubility: 100 mg/mL (260.77 mM); Clear solution; Need ultrasonic

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

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    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Calculation results:
    Working solution concentration: mg/mL
    This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
    Purity & Documentation
    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 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

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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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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