Bisoprolol hemifumarate
Based on 6 publication(s) in Google Scholar
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.
- Purity: 99.84%
- CAS No.: 104344-23-2
- Formula: C18H31NO4.1/2C4H4O4
- Molecular Weight:383.48
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications Citing Use of MedChemExpress (MCE) Bisoprolol hemifumarate
More- Cell Rep. 2024 May 31;43(6):114302. [Abstract]
- Int J Mol Sci. 2023 Aug 9;24(16):12609. [Abstract]
- Mol Neurobiol. 2019 Jan;56(1):367-377. [Abstract]
- Am J Respir Cell Mol Biol. 2023 Aug;69(2):230-241. [Abstract]
- ACS Omega. 2022 Aug 8;7(32):27950-27958. [Abstract]
- J Pharm Biomed Anal. 2021 Feb 20:195:113870. [Abstract]
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WB
All Adrenergic Receptor Isoforms
More
Biological Activity
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Beta-1 adrenergic receptor |
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.
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Cell Line:H9c2 cells
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Concentration:0.2, 2, 20 μM
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Incubation Time:1 h
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Result:Elevated the survival rates of cardiomyocytes subjected to H/R (hypoxia/reoxygenation) to 73.20%, 90.38%, 81.25% respectively.
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Cell Line:DCs
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Concentration:100 μM
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Incubation Time:6, 12, 24 h
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Result:Increased the amount of migrating cells by 46.00% (6 h), 64.25% (12 h) and 55.74% (24 h).
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.
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Animal Model:Ischemia/reperfusion (I/R) injury rats[2]
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Dosage:0.5, 5, 10 mg/kg
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Administration:Oral administration, for 1 week, prior to 0.5 h ischemia/4 h reperfusion.
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Result:Reduced infarct size from 44% in I/R group to 31% in treated group.
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Animal Model:Cadmium-induced rats[4]
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Dosage:2, 8 mg/kg
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Administration:Oral gavage, daily for four weeks.
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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.
Chemical Information
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CAS No. 104344-23-2
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Appearance Solid
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Molecular Weight 383.48
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Formula C18H31NO4.1/2C4H4O4
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Color White to off-white
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SMILES
OC(CNC(C)C)COC1=CC=C(COCCOC(C)C)C=C1.OC(/C=C/C(O)=O)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (6)
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Journal Impact Factor
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Most Recent
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Cell Rep
2024 May 31;43(6):114302. PMID: 38824644 -
Int J Mol Sci
Elevated Blood Pressure Occurs without Endothelial Dysfunction in a Rat Model of Pulmonary Emphysema. [Abstract]2023 Aug 9;24(16):12609. PMID: 37628790 -
Mol Neurobiol
Identification of Alprenolol Hydrochloride as an Anti-prion Compound Using Surface Plasmon Resonance Imaging. [Abstract]2019 Jan;56(1):367-377. PMID: 29704200
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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Am J Respir Cell Mol Biol
2023 Aug;69(2):230-241. PMID: 37163759 -
ACS Omega
Computational and Experimental Approaches Identify Beta-Blockers as Potential SARS-CoV-2 Spike Inhibitors. [Abstract]2022 Aug 8;7(32):27950-27958. PMID: 35983371 -
J Pharm Biomed Anal
Screening method of mildronate and over 300 doping agents by reversed-phase liquid chromatography-high resolution mass spectrometry. [Abstract]2021 Feb 20:195:113870. PMID: 33453569
Solvent & Solubility
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.
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- 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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 5 mg/mL (13.04 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 5 mg/mL (13.04 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
Add each solvent one by one: PBS
Solubility: 100 mg/mL (260.77 mM); Clear solution; Need ultrasonic
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.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Purity & Documentation
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Data Sheet (279 KB)
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SDS (557 KB)
- English - EN (557 KB)
- Français - FR (557 KB)
- Deutsch - DE (557 KB)
- Norwegian - NO (557 KB)
- Español - ES (557 KB)
- Swedish - SV (557 KB)
- Italian - IT (557 KB)
- Korean - KR (557 KB)
- Portuguese - PT (557 KB)
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Handling Instructions (2659 KB)
References
[1]. Jillian G Baker, et al. The selectivity of beta-adrenoceptor antagonists at the human beta1, beta2 and beta3 adrenoceptors. Br J Pharmacol. 2005 Feb;144(3):317-22. [Content Brief]
[2]. Jing Wang, et al. Bisoprolol, a β 1 antagonist, protects myocardial cells from ischemia-reperfusion injury via PI3K/AKT/GSK3β pathway. Fundam Clin Pharmacol. 2020 Dec;34(6):708-720. [Content Brief]
[3]. Hong Yang, et al. Bisoprolol reverses epinephrine-mediated inhibition of cell emigration through increases in the expression of β-arrestin 2 and CCR7 and PI3K phosphorylation, in dendritic cells loaded with cholesterol. Thromb Res. 2013 Mar;131(3):230-7. [Content Brief]
[4]. Jinhua Liu, et al. Protective Effects of Bisoprolol Against Cadmium-induced Myocardial Toxicity Through Inhibition of Oxidative Stress and NF-κΒ Signalling in Rats. J Vet Res. 2021 Oct 20;65(4):505-511. [Content Brief]
[5]. Yajuan Ni, et al. Bisoprolol reversed small conductance calcium-activated potassium channel (SK) remodeling in a volume-overload rat model. Mol Cell Biochem. 2013 Dec;384(1-2):95-103. [Content Brief]
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.