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| 250mg |
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Purity: ≥98%
Bisoprolol fumarate (Zebeta; (+/-)-Bisoprolol hemifumarate; Bisobloc; EMD 33512; EMD33512), the fumarate salt of bisoprolol, is a potent and selective β1 adrenergic receptor antagonist/blocker with potentialantihypertensiveand cardioprotective activities. It has been applied to the treatment of angina pectoris and hypertension.
| Targets |
β1-adrenergic receptor
|
|---|---|
| ln Vitro |
Bisoprolol fumarate (2 μM, 1 h) shields myocardial cells (H9c2) from ischemia/reperfusion (I/R) injury[2].
Bisoprolol fumarate (2 μM, 1 h) decreases ROS production and apoptosis brought on by H/R in H9c2 cells[2]. Bisoprolol fumarate (2 μM, 1 h) raises AKT and GSK3β phosphorylation in H9c2 cells[2]. Bisoprolol fumarate (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 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].
Bisoprolol fumarate (oral gavage, 8 mg/kg, daily for four weeks) exhibits protective effects against rats' myocardial toxicity caused by cadmium[4]. Bisoprolol fumarate (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 |
chemia/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 |
|
| Molecular Formula |
C40H66N2O12
|
|---|---|
| Molecular Weight |
766.9583
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| Exact Mass |
766.46
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| Elemental Analysis |
C, 62.64; H, 8.67; N, 3.65; O, 25.03
|
| CAS # |
104344-23-2
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| Related CAS # |
Bisoprolol fumarate; 105878-43-1; Bisoprolol; 66722-44-9; Bisoprolol-d7 hemifumarate
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| Appearance |
Solid powder
|
| SMILES |
CC(C)NCC(COC1=CC=C(C=C1)COCCOC(C)C)O.CC(C)NCC(COC1=CC=C(C=C1)COCCOC(C)C)O.C(=C/C(=O)O)\C(=O)O
|
| InChi Key |
VMDFASMUILANOL-WXXKFALUSA-N
|
| InChi Code |
InChI=1S/2C18H31NO4.C4H4O4/c2*1-14(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/h2*5-8,14-15,17,19-20H,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
|
| Synonyms |
EMD-33512; Bisoprolol hemifumarate; Bisoprolol hemifumarate salt; Zebeta; (+/-)-Bisoprolol hemifumarate; Bisobloc; EMD 33512; EMD33512
|
| 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 Vitro) |
DMSO: ~88 mg/mL (~199.3 mM)
Water: ~88 mg/mL (~199.3 mM) Ethanol: ~88 mg/mL (~199.3 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 100 mg/mL (260.77 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.3038 mL | 6.5192 mL | 13.0385 mL | |
| 5 mM | 0.2608 mL | 1.3038 mL | 2.6077 mL | |
| 10 mM | 0.1304 mL | 0.6519 mL | 1.3038 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 |
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