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Bisoprolol fumarate

Cat No.:V43677 Purity: ≥98%
Bisoprolol fumarate is a potent, selective, orally bioactive β1-adrenergic receptor blocker (antagonist) (blocker) with minimal activity at β2 receptors.
Bisoprolol fumarate
Bisoprolol fumarate Chemical Structure CAS No.: 105878-43-1
Product category: New3
This product is for research use only, not for human use. We do not sell to patients.
Size Price
500mg
1g
Other Sizes

Other Forms of Bisoprolol fumarate:

  • Bisoprolol fumarate
  • Bisoprolol-d5 hemifumarate
  • Bisoprolol-d7 hemifumarate (Bisoprolol d7 (hemifumarate))
  • Bisoprolol-d6 hemifumarate
  • Bisoprolol-d5 (Bisoprolol-d5)
  • Bisoprolol-d7
  • Bisoprolol
Official Supplier of:
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Top Publications Citing lnvivochem Products
Product Description
Bisoprolol fumarate is a potent, selective, orally bioactive β1-adrenergic receptor blocker (antagonist) (blocker) with minimal activity at β2 receptors. Bisoprolol fumarate is indicated for the study of hypertension, coronary artery disease, and stable ventricular dysfunction.
Biological Activity I Assay Protocols (From Reference)
ln Vitro
Ischemia/reperfusion (I/R) injury is prevented in cardiomyocytes (H9c2) by bisoprolol fumarate (2 μM, 1 hour) [2]. In H9c2 cells, bisoprolol fumarate (2 μM, 1 h) can lessen ROS production and apoptosis brought on by H/R [2]. In H9c2 cells, bisoprolol fumarate (2 μM, 1 hour) raises AKT and GSK3β phosphorylation [2]. By increasing β-arrestin 2, CCR7, and PI3K phosphorylation, bisoprolol fumarate (100 μM, 24 hours) reverses the effects of epinephrine-inhibited migration in cholesterol-loaded DCs (dendritic cells) [3]. Determination of cell viability [2]
ln Vivo
Bisoprolol fumarate lowers heart rate and raises left ventricular ejection fraction (LVEF) when taken orally for one week at a dose of 5 mg/kg [2]. Administering bisoprolol fumarate orally (daily, 8 mg/kg) for four weeks has been shown to protect rats from cadmium-induced cardiotoxicity [4]. In a rat model of volume overload, bisoprolol fumarate (oral gavage, 1 mg/kg daily for 6 weeks) reverses small-conductance calcium-activated potassium channel (SK) remodeling [5].
Cell Assay
Cell viability determination [2]
Cell Types: H9c2 Cell
Tested Concentrations: 0.2, 2, 20 μM
Incubation Duration: 1 h
Experimental Results: H/R (hypoxia/reoxygenation) cardiomyocyte survival rate increased to 73.20%, 90.38%, 81.25% respectively.

Cell migration assay [3]
Cell Types: DC
Tested Concentrations: 100 μM
Incubation Duration: 6, 12, 24 hrs (hours)
Experimental Results: The number of migrating cells increased by 46.00% (6 hrs (hours)), 64.25% (12 hrs (hours)), and 55.74% (24 H).
Animal Protocol
Animal/Disease Models: ischemia/reperfusion (I/R) injury in rats [2]
Doses: 0.5, 5, 10 mg/kg
Route of Administration: Oral administration for 1 week, after 0.5 hrs (hrs (hours)) of ischemia/4 hrs (hrs (hours)) of re-injury before perfusion.
Experimental Results: Infarct size diminished from 44% in the I/R group to 31% in the treatment group.

Animal/Disease Models: Cadmium-induced rats [4]
Doses: 2, 8 mg/kg
Route of Administration: po (oral gavage), one time/day for four weeks.
Experimental Results: Mean arterial pressure (MAP) diminished to 8 mg/kg. Serum biomarkers (ALT, AST) and NF-kB p65 expression as well as TNF-α levels (cardiac tissue samples) were diminished at 8 mg/kg.
References

[1]. The selectivity of beta-adrenoceptor antagonists at the human beta1, beta2 and beta3 adrenoceptors. Br J Pharmacol. 2005 Feb;144(3):317-22.

[2]. 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.

[3]. 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.

[4]. 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.

[5]. 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.

Additional Infomation
Bisoprolol Fumarate is the fumarate salt of a synthetic phenoxy-2-propanol-derived cardioselective beta-1 adrenergic receptor antagonist with antihypertensive and potential cardioprotective activities. Devoid of intrinsic sympathomimetic activity, bisoprolol selectively and competitively binds to and blocks beta-1 adrenergic receptors in the heart, decreasing cardiac contractility and rate, reducing cardiac output, and lowering blood pressure. In addition, this agent may exhibit antihypertensive activity through the inhibition of renin secretion by juxtaglomerular epithelioid (JGE) cells in the kidney, thus inhibiting activation of the renin-angiotensin system (RAS). Bisoprolol has been shown to be cardioprotective in animal models.
A cardioselective beta-1 adrenergic blocker. It is effective in the management of HYPERTENSION and ANGINA PECTORIS.
See also: Bisoprolol (annotation moved to); Bisoprolol Fumarate (annotation moved to).
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C22H35NO8
Molecular Weight
441.515207529068
Exact Mass
441.236
CAS #
105878-43-1
Related CAS #
Bisoprolol hemifumarate;104344-23-2;Bisoprolol-d5 hemifumarate;Bisoprolol;66722-44-9
PubChem CID
6917733
Appearance
Typically exists as solid at room temperature
Hydrogen Bond Donor Count
4
Hydrogen Bond Acceptor Count
9
Rotatable Bond Count
14
Heavy Atom Count
31
Complexity
397
Defined Atom Stereocenter Count
0
SMILES
CC(C)NCC(COC1=CC=C(C=C1)COCCOC(C)C)O.C(=C/C(=O)O)\C(=O)O
InChi Key
RZPZLFIUFMNCLY-WLHGVMLRSA-N
InChi Code
InChI=1S/C18H31NO4.C4H4O4/c1-14(2)19-11-17(20)13-23-18-7-5-16(6-8-18)12-21-9-10-22-15(3)4;5-3(6)1-2-4(7)8/h5-8,14-15,17,19-20H,9-13H2,1-4H3;1-2H,(H,5,6)(H,7,8)/b;2-1+
Chemical Name
(E)-but-2-enedioic acid;1-(propan-2-ylamino)-3-[4-(2-propan-2-yloxyethoxymethyl)phenoxy]propan-2-ol
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
Solubility (In Vivo)
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.

Injection Formulations
(e.g. IP/IV/IM/SC)
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution 50 μL Tween 80 850 μL Saline)
*Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution.
Injection Formulation 2: DMSO : PEG300Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO 400 μLPEG300 50 μL Tween 80 450 μL Saline)
Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO 900 μL Corn oil)
Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals).
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Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO 900 μL (20% SBE-β-CD in saline)]
*Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO 100 μLPEG300 200 μL castor oil 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10: 10 : 80 (i.e. 100 μL Ethanol 100 μL Cremophor 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH 400 μLPEG300 50 μL Tween 80 450 μL Saline)


Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium)
Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose
Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals).
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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders


Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.2649 mL 11.3245 mL 22.6490 mL
5 mM 0.4530 mL 2.2649 mL 4.5298 mL
10 mM 0.2265 mL 1.1325 mL 2.2649 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

  • Calculate the Mass of a compound required to prepare a solution of known volume and concentration
  • Calculate the Volume of solution required to dissolve a compound of known mass to a desired concentration
  • Calculate the Concentration of a solution resulting from a known mass of compound in a specific volume
An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
  • Enter 350.26 in the Molecular Weight (MW) box
  • Enter 10 in the Concentration box and choose the correct unit (mM)
  • Enter 5 in the Volume box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
  • Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
  • Enter 25 into the Concentration (End) box and select the correct unit (mM)
  • Enter 25 into the Volume (End) box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:
  • To calculate molar mass of a chemical compound, please enter the chemical/molecular formula and click the “Calculate’ button.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
  • Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
  • Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

  • Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
  • Click the “Calculate” button
  • The answer appears in the Volume (to add to vial) box
In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

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Date: 2024-10-16
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CTID: NCT05536284
Phase: Phase 2    Status: Completed
Date: 2023-06-07
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CTID: NCT03779646
Phase: Phase 2/Phase 3    Status: Unknown status
Date: 2022-09-28
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Evaluation of the Clinical Efficacy and Safety of Amlodipine 5mg/ Bisoprolol Fumarate 5mg /Perindopril Arginine 5mg Fixed-dose Combination in Capsule and Free Monotherapy at the Same Dose in Patients With Uncontrolled Essential Hypertension.
CTID: NCT05288400
Phase: Phase 3    Status: Completed
Date: 2022-08-05


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Date: 2022-03-10
Effect of Amlodipine Versus Bisoprolol on Hypertensive Patients With End-stage Renal Disease on Maintenance Hemodialysis.
CTID: NCT04085562
Phase: Phase 4    Status: Completed
Date: 2021-02-17
Bioequivalence Study of Bisoprolol Fumarate Tablet 10 mg Under Fed Condition
CTID: NCT01744873
Phase: Phase 1    Status: Completed
Date: 2012-12-07
Bioequivalence Study of Bisoprolol Fumarate
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