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Bucindolol

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Catalog No. T10631Cas No. 71119-11-4
Alias MJ 131051, MJ 13105, BMY 13105

Bucindolol (BMY 13105) is a novel and potent β1-adrenergic receptor blocker that mediates vasodilation and can be used to study chronic heart failure.

Bucindolol

Bucindolol

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Purity: 99.9%
Catalog No. T10631Alias MJ 131051, MJ 13105, BMY 13105Cas No. 71119-11-4
Bucindolol (BMY 13105) is a novel and potent β1-adrenergic receptor blocker that mediates vasodilation and can be used to study chronic heart failure.
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1 mg$39In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:99.9%
Appearance:Solid
Color:White
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Product Introduction

Bucindolol AI Summary
Bucindolol exhibits a wide range of bioactivities across various biological systems. It acts as a beta-adrenergic receptor blocker in normotensive rats, achieving 71.0% inhibition at 2 mg/kg, and demonstrates intrinsic sympathomimetic activity with 77.0 beats per minute in reserpinized rats. Additionally, it shows antihypertensive effects in spontaneously hypertensive rats with a 45.0 mmHg reduction in blood pressure following peroral administration and possesses vasodilator activity in ganglion-blocked rats, leading to a 26.0% decrease in mean arterial blood pressure at 3 mg/kg intravenously. Bucindolol is a potent inhibitor of the enzyme Cytochrome P450 2D6 (CYP2D6), with an IC50 value of 50.0 nM after 45 minutes of incubation. It also significantly inhibits the uptake of 4-(4-(dimethylamino)styryl)-N-methylpyridinium via human OCT1 in HEK293 cells, with an IC50 of 27,200.0 nM and 84.6% inhibition at a concentration of 100 µM. The compound shows diverse bioactivity in various other assays, including inhibition of the Menin-MLL interaction in MLL-related leukemias, GCN5L2 inhibition, delayed death inhibition of the malarial parasite plastid, and Schwann cell viability assays. Additionally, it induces DNA re-replication in SW480 colon adenocarcinoma cells, inhibits human tyrosyl-DNA phosphodiesterase 1 (TDP1), blocks viral entries, including Lassa Virus, Marburg Virus, Ebola Virus, and SARS-CoV-2, with an IC50 ranging from 16,982.44 nM to 17,000.0 nM for SARS-CoV-2. The compound also inhibits insulin secretion from INS-1E cells at different glucose concentrations, with varying potencies in the nanomolar and micromolar ranges. Lastly, Bucindolol exhibits antiviral activity against SARS-CoV-2 in VERO-E6 cells, demonstrating an IC50 range of 16,982.44 nM to 17,000.0 nM and a CC50 value of 30,900.0 nM, indicating both its potency and certain cytotoxicity to VERO-E6 cells..
Note: Summary generated by AI. Data source: ChEMBL
Bioactivity
Description
Bucindolol (BMY 13105) is a novel and potent β1-adrenergic receptor blocker that mediates vasodilation and can be used to study chronic heart failure.
SynonymsMJ 131051, MJ 13105, BMY 13105
Chemical Properties
Molecular Weight363.45
FormulaC22H25N3O2
Cas No.71119-11-4
SmilesCC(C)(Cc1c[nH]c2ccccc12)NCC(O)COc1ccccc1C#N
Relative Density.1.31g/cm3
Storage & Solubility Information
Storagestore at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 80 mg/mL (220.11 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.7514 mL13.7571 mL27.5141 mL137.5705 mL
5 mM0.5503 mL2.7514 mL5.5028 mL27.5141 mL
10 mM0.2751 mL1.3757 mL2.7514 mL13.7571 mL
20 mM0.1376 mL0.6879 mL1.3757 mL6.8785 mL
50 mM0.0550 mL0.2751 mL0.5503 mL2.7514 mL
100 mM0.0275 mL0.1376 mL0.2751 mL1.3757 mL

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Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
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2 Enter the in vivo formulation:
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