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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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1g |
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Purity: ≥98%
Bisoprolol (also known as EMD33512) is a potent and selective type β1 adrenergic receptor blocker. It works well for treating angina pectoris and hypertension. Hemifumarate, or bisoprolol, has antihypertensive and possibly cardioprotective properties. Bisoprolol, which lacks intrinsic sympathomimetic activity, selectively and competitively binds to and blocks beta-1 adrenergic receptors in the heart, lowering blood pressure, cardiac output, and contractility and rate.
Targets |
Beta-1 adrenergic receptor
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ln Vitro |
Bisoprolol (2 μM, 1 h) shields myocardial cells (H9c2) from ischemia/reperfusion (I/R) injury[2].
Bisoprolol (2 μM, 1 h) decreases ROS production and apoptosis caused by H/R in H9c2 cells[2]. Bisoprolol (2 μM, 1 h) raises AKT and GSK3β phosphorylation in H9c2 cells[2]. Bisoprolol (100 μM, 24 h) increases β-arrestin 2, CCR7, and PI3K phosphorylation, which reverses the effects of epinephrine-inhibited emigration in cholesterol-loaded DCs (dendritic cells)[3]. |
ln Vivo |
Bisoprolol (oral administration, 5 mg/kg, for 1 week) lowers heart rate and raises left ventricular ejection fraction (LVEF)[2].
Bisoprolol (oral gavage, 8 mg/kg, daily for four weeks) protects against cadmium-induced myocardial toxicity in rats[4]. Bisoprolol (oral gavage, 1 mg/kg, daily for 6 weeks) (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]. |
Cell Assay |
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. |
Animal Protocol |
Ischemia/reperfusion (I/R) injury rats
0.5, 5, 10 mg/kg Oral administration, for 1 week, prior to 0.5 h ischemia/4 h reperfusion. |
References |
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Molecular Formula |
C18H31NO4
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Molecular Weight |
325.44
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Exact Mass |
325.23
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Elemental Analysis |
C, 66.43; H, 9.60; N, 4.30; O, 19.66
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CAS # |
66722-44-9
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Related CAS # |
Bisoprolol-d5; 1189881-87-5; Bisoprolol hemifumarate; 104344-23-2; Bisoprolol fumarate; 105878-43-1
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Appearance |
Solid powder
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SMILES |
CC(C)NCC(COC1=CC=C(C=C1)COCCOC(C)C)O
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InChi Key |
VHYCDWMUTMEGQY-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C18H31NO4/c1-14(2)19-11-17(20)13-23-18-7-5-16(6-8-18)12-21-9-10-22-15(3)4/h5-8,14-15,17,19-20H,9-13H2,1-4H3
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Chemical Name |
1-(propan-2-ylamino)-3-[4-(2-propan-2-yloxyethoxymethyl)phenoxy]propan-2-ol
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Synonyms |
CL297,939; CL-297,939; Bisoprolol; CL 297,939
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HS Tariff Code |
2934.99.9001
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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)
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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
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *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 : PEG300 :Tween 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). View More
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)] 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). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
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Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 3.0728 mL | 15.3638 mL | 30.7276 mL | |
5 mM | 0.6146 mL | 3.0728 mL | 6.1455 mL | |
10 mM | 0.3073 mL | 1.5364 mL | 3.0728 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.
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.
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT03278509 | Active Recruiting |
Drug: Metoprolol Succinate Drug: Bisoprolol |
Acute Myocardial Infarction ST Elevation Myocardial Infarction |
Karolinska Institutet | September 11, 2017 | Phase 4 |
NCT03917914 | Active Recruiting |
Drug: Bisoprolol Drug: Placebo Oral Tablet |
Cardiovascular Diseases Chronic Obstructive Pulmonary Disease |
The George Institute | June 30, 2020 | Phase 3 |
NCT05794997 | Active Recruiting |
Drug: Propranolol or Carvedilol Drug: Atenolol, Bisoprolol or Sotalol |
Hypertension | Brigham and Women's Hospital | November 30, 2022 | N/A |
NCT05540600 | Recruiting | Drug: Digoxin 0.25 mg Drug: Bisoprolol |
Atrial Fibrillation Left Atrial Rhythm |
University of Monastir | September 12, 2022 | Phase 3 |
NCT05294887 | Recruiting | Drug: Bisoprolol Drug: Diltiazem Drug: Placebo |
Microvascular Angina Vasospastic Angina Prinzmetal Angina |
Charite University, Berlin, Germany |
March 4, 2022 | Phase 4 |
Serum creatine kinase-MB (CK-MB) levels in rats treated with cadmium and bisoprolol (BIS) (2 and 8 mg/kg/day). J Vet Res . 2021 Oct 20;65(4):505-511. td> |
Serum lactic acid dehydrogenase (LDH) levels in rats treated with cadmium and bisoprolol (BIS) (2 and 8 mg/kg/day). J Vet Res . 2021 Oct 20;65(4):505-511. td> |