Bisoprolol
Based on 6 publication(s) in Google Scholar
Bisoprolol is a potent, selective and orally active β1-adrenergic receptor blocker with little activity on β2-receptor. Bisoprolol has the potential for hypertension, coronary artery disease and stable ventricular dysfunction research.
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- Pureté: 99.78%
- CAS No.: 66722-44-9
- Formule: C18H31NO4
- Masse moléculaire:325.44
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Stockage:Pure form -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
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Publications Citing Use of MedChemExpress (MCE) Bisoprolol
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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Activité biologique
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Beta-1 adrenergic receptor |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A-375 | IC50 |
>100 μM
Compound: Bisoprolol
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Antiproliferative activity against human A375 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay
Antiproliferative activity against human A375 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay
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[PMID: 32216987] |
| SK-MEL-28 | IC50 |
>100 μM
Compound: Bisoprolol
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Antiproliferative activity against human SK-MEL-28 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay
Antiproliferative activity against human SK-MEL-28 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay
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[PMID: 32216987] |
| SK-MEL-5 | IC50 |
>100 μM
Compound: Bisoprolol
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Antiproliferative activity against human SK-MEL-5 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay
Antiproliferative activity against human SK-MEL-5 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay
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[PMID: 32216987] |
Bisoprolol (2 μM, 1 h) protects myocardial cells (H9c2) from ischemia/reperfusion (I/R) injury[2].
Bisoprolol (2 μM, 1 h) reduces the H/R-induced ROS production and apoptosis in H9c2 cells[2].
Bisoprolol (2 μM, 1 h) increases AKT and GSK3β phosphorylation in H9c2 cells[2].
Bisoprolol (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 (oral gavage, 8 mg/kg, daily for four weeks) shows protective effects against Cadmium-induced myocardial toxicity in rats[4].
Bisoprolol (oral gavage, 1 mg/kg, daily for 6 weeks) reverses small 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. 66722-44-9
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Appearance Liquid (Density: 1.033±0.06 g/cm3)
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Masse moléculaire 325.44
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Formule C18H31NO4
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Color Colorless to light yellow
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SMILES
OC(CNC(C)C)COC1=CC=C(COCCOC(C)C)C=C1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Pure form -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
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 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
Solvant et solubilité
DMSO : 175 mg/mL (537.73 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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: ≥ 2.5 mg/mL (7.68 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (7.68 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
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.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureté et documentation
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Fiche technique (276 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instruction de manipulation (2659 KB)
Références
[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. 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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.0728 mL | 15.3638 mL | 30.7276 mL | 76.8191 mL |
| 5 mM | 0.6146 mL | 3.0728 mL | 6.1455 mL | 15.3638 mL | |
| 10 mM | 0.3073 mL | 1.5364 mL | 3.0728 mL | 7.6819 mL | |
| 15 mM | 0.2049 mL | 1.0243 mL | 2.0485 mL | 5.1213 mL | |
| 20 mM | 0.1536 mL | 0.7682 mL | 1.5364 mL | 3.8410 mL | |
| 25 mM | 0.1229 mL | 0.6146 mL | 1.2291 mL | 3.0728 mL | |
| 30 mM | 0.1024 mL | 0.5121 mL | 1.0243 mL | 2.5606 mL | |
| 40 mM | 0.0768 mL | 0.3841 mL | 0.7682 mL | 1.9205 mL | |
| 50 mM | 0.0615 mL | 0.3073 mL | 0.6146 mL | 1.5364 mL | |
| 60 mM | 0.0512 mL | 0.2561 mL | 0.5121 mL | 1.2803 mL | |
| 80 mM | 0.0384 mL | 0.1920 mL | 0.3841 mL | 0.9602 mL | |
| 100 mM | 0.0307 mL | 0.1536 mL | 0.3073 mL | 0.7682 mL |
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