| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg | |||
| 50mg | |||
| 100mg | |||
| Other Sizes |
| Targets |
Bucindolol targets β₁- and β₂-adrenergic receptors, acting as a blocker. It also exhibits alpha-adrenergic antagonism, contributing to its vasodilatory properties. As a β₁-adrenergic receptor blocker, it reduces heart rate and myocardial oxygen demand, which can be beneficial in heart failure. Its intrinsic sympathomimetic activity may provide additional benefits by preventing excessive bradycardia. The compound's multi-targeted mechanism of action, including beta-blockade and vasodilation, makes it a unique agent for cardiovascular research.
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| ln Vitro |
In vitro, Bucindolol is a β₁-adrenergic receptor blocker. Its activity is typically assessed by measuring its binding affinity to β₁- and β₂-adrenergic receptors using radioligand binding studies. Its functional activity as a blocker is assessed by measuring its ability to inhibit isoproterenol-stimulated cAMP accumulation in cells expressing these receptors. Its alpha-adrenergic antagonism can be assessed by measuring its effects on vasoconstriction.
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| ln Vivo |
In vivo, Bucindolol has been investigated in heart failure. Its beta-blocking and vasodilatory properties make it a potential therapeutic agent for heart failure. However, its clinical development has been limited. The compound has a maximum clinical trial phase of II. Its effects on heart rate, blood pressure, and cardiac function have been studied in clinical trials.
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| Enzyme Assay |
In vitro non-cell enzyme/receptor binding assays for Bucindolol involve measuring its binding affinity to β₁- and β₂-adrenergic receptors. Radioligand binding studies using membrane preparations and a labeled ligand (e.g., [³H]CGP-12177) are used to determine its affinity (Ki). Functional assays, such as measuring its ability to inhibit isoproterenol-stimulated cAMP production in a cell-free system, are used to determine its activity as a blocker.
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| Cell Assay |
In vitro cell-based assays for Bucindolol use cell lines expressing β₁- and β₂-adrenergic receptors. Cells are treated with varying concentrations of the compound, and cAMP levels are measured to assess its ability to block isoproterenol-stimulated cAMP accumulation. Its effects on cell viability and signaling pathways can also be studied. These studies help to characterize the compound's cellular mechanism of action.
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| Animal Protocol |
In vivo animal studies for Bucindolol employ models of heart failure, such as the rat or dog model of heart failure. The compound is administered, and parameters such as heart rate, blood pressure, cardiac output, and survival are assessed. Its effects on cardiac remodeling and function are evaluated by echocardiography and histopathology. Pharmacokinetic studies in these models provide information about the compound's absorption, distribution, metabolism, and excretion.
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| ADME/Pharmacokinetics |
Bucindolol has a molecular weight of 363.45 g/mol and a molecular formula of C₂₂H₂₅N₃O₂. It is also known as MJ 13105-1. The compound appears as white crystals with a melting point of 125-127°C. It should be stored under appropriate conditions, typically at room temperature, protected from light and moisture. Its pharmacokinetic profile supports oral administration.
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| Toxicity/Toxicokinetics |
Bucindolol is generally well-tolerated, but side effects can include bradycardia, hypotension, and fatigue. It is contraindicated in patients with a history of hypersensitivity to Bucindolol or any of its components. Its use during pregnancy and lactation is not recommended due to insufficient safety data.
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| References |
Black-Maier E, Steinberg BA, Piccini JP. Bucindolol hydrochloride in atrial fibrillation and concomitant heart failure. Expert Rev Cardiovasc Ther. 2015 Jun;13(6):627-36. doi: 10.1586/14779072.2015.1031111. Epub 2015 May 11. Review. PubMed PMID: 25959096.
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| Additional Infomation |
Bucindolol has been used in research to treat heart failure.
Bucindolol is a β₁-adrenergic receptor blocker with intrinsic sympathomimetic activity, used in the research of heart failure. It also exhibits vasodilatory properties through alpha-adrenergic antagonism. It has been investigated in heart failure. Not approved for clinical use in many countries; intended for research purposes only. |
| Molecular Formula |
C₂₂H₂₅N₃O₂
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|---|---|
| Molecular Weight |
363.4528
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| Exact Mass |
363.194
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| CAS # |
71119-11-4
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| Related CAS # |
71119-11-4 70369-47-0 (HCl) |
| PubChem CID |
51045
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| Appearance |
White to off-white solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
605.3±55.0 °C at 760 mmHg
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| Flash Point |
319.9±31.5 °C
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| Vapour Pressure |
0.0±1.8 mmHg at 25°C
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| Index of Refraction |
1.632
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| LogP |
3.19
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
27
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| Complexity |
515
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
FBMYKMYQHCBIGU-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H25N3O2/c1-22(2,11-17-13-24-20-9-5-4-8-19(17)20)25-14-18(26)15-27-21-10-6-3-7-16(21)12-23/h3-10,13,18,24-26H,11,14-15H2,1-2H3
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| Chemical Name |
2-[2-Hydroxy-3-[[2-(1H-indol-3-yl)-1,1-dimethylethyl]amino]propoxy]benzonitrile
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| Synonyms |
MJ-131051 MJ 131051 MJ131051 MJ-13105-1 MJ 13105-1 DL-Bucindolol
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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 Vitro) |
DMSO : ~100 mg/mL (~275.14 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (6.88 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.88 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. 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. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.88 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7514 mL | 13.7571 mL | 27.5141 mL | |
| 5 mM | 0.5503 mL | 2.7514 mL | 5.5028 mL | |
| 10 mM | 0.2751 mL | 1.3757 mL | 2.7514 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.
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