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Bufuralol hydrochloride (Synonyms: Ro 3-4787 hydrochloride, Bufuralol hydrochloride)

Name: Bufuralol hydrochloride
Brand: TargetMol
SKU: T21684
Rating: 4.5 (1 reviews)

Catalog No. T21684 Copy Product Info

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Bufuralol hydrochloride belongs to the class of beta-adrenoreceptor antagonists and is a potent, orally active, non-selective beta-adrenoreceptor antagonist with partial agonist activity. Bufuralol hydrochloride is a prototypical CYP2D6 probe substrate (Km = 5-50 microM) and is extensively used in biochemical studies to characterize CYP2D6 enzymatic activity and evaluate genetic variants.

Bufuralol hydrochloride

Copy Product Info

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Catalog No. T21684

Synonyms Ro 3-4787 hydrochloride, Bufuralol hydrochloride

Cas No. 60398-91-6

Pack Size	Price	USA Stock	Global Stock
1 mg	$461	35 days	35 days
5 mg	$1,015	35 days	35 days
10 mg	Inquiry	35 days	35 days

For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)

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For research use only—not for human use. No sales to individuals. Use as intended only.

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Appearance:Solid

Color:White

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COA

Product Introduction

Bioactivity

Description	Bufuralol hydrochloride belongs to the class of beta-adrenoreceptor antagonists and is a potent, orally active, non-selective beta-adrenoreceptor antagonist with partial agonist activity. Bufuralol hydrochloride is a prototypical CYP2D6 probe substrate (Km = 5-50 microM) and is extensively used in biochemical studies to characterize CYP2D6 enzymatic activity and evaluate genetic variants.
In vitro	Bufuralol hydrochloride, featuring characteristic CYP2D6 substrate motifs, is used in vitro to evaluate the metabolic kinetics of CYP2D6 variants. Studies show an apparent Km of approximately 5 microM for bufuralol 1'-hydroxylation by recombinant CYP2D6[1].
In vivo	In vivo,Bufuralol hydrochloride metabolism is NADPH-mediated and exhibits biphasic kinetics. Its metabolic profile in rhesus monkey intestines is consistent with liver observations, facilitating the evaluation of systemic and local CYP2D6 metabolic efficiency[1].
Synonyms	Ro 3-4787 hydrochloride, Bufuralol hydrochloride

Chemical Properties

Molecular Weight	297.82
Formula	C₁₆H₂₄ClNO₂
Cas No.	60398-91-6
Smiles	Cl.OC(C=1OC2=C(C=CC=C2CC)C1)CNC(C)(C)C
Relative Density.	no data available

Storage & Solubility Information

Storage

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 (268.62 mM), Sonication is recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	3.3577 mL	16.7887 mL	33.5773 mL	167.8866 mL
5 mM	0.6715 mL	3.3577 mL	6.7155 mL	33.5773 mL
10 mM	0.3358 mL	1.6789 mL	3.3577 mL	16.7887 mL
20 mM	0.1679 mL	0.8394 mL	1.6789 mL	8.3943 mL
50 mM	0.0672 mL	0.3358 mL	0.6715 mL	3.3577 mL
100 mM	0.0336 mL	0.1679 mL	0.3358 mL	1.6789 mL

Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

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In Vivo Formulation Calculator (Clear solution)

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:

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 DMSO TargetMol | 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 DMSO TargetMol | reagent stock solution to 400 μL PEG300 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 ddH₂O TargetMol | 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.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc