Bisoprolol fumarate
Based on 6 publication(s) in Google Scholar
Bisoprolol fumarate is a potent, selective and orally active β1-adrenergic receptor blocker with little activity on β2-receptor. Bisoprolol fumarate has the potential for hypertension, coronary artery disease and stable ventricular dysfunction research.
For research use only. We do not sell to patients.
- CAS No.: 105878-43-1
- Formula: C22H35NO8
- Molecular Weight:441.52
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
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Publications Citing Use of MedChemExpress (MCE) Bisoprolol fumarate
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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All Adrenergic Receptor Isoforms
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Biological Activity
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Beta-1 adrenergic receptor |
Bisoprolol fumarate (2 μM, 1 h) protects myocardial cells (H9c2) from ischemia/reperfusion (I/R) injury[2].
Bisoprolol fumarate (2 μM, 1 h) reduces the H/R-induced ROS production and apoptosis in H9c2 cells[2].
Bisoprolol fumarate (2 μM, 1 h) increases AKT and GSK3β phosphorylation in H9c2 cells[2].
Bisoprolol fumarate (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 fumarate (oral gavage, 8 mg/kg, daily for four weeks) shows protective effects against Cadmium-induced myocardial toxicity in rats[4].
Bisoprolol fumarate (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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 105878-43-1
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Molecular Weight 441.52
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Formula C22H35NO8
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SMILES
OC(COC1=CC=C(C=C1)COCCOC(C)C)CNC(C)C.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
Please store the product under the recommended conditions in the Certificate of Analysis.
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 fumarate 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
Purity & Documentation
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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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