2. GPCR/G Protein Neuronal Signaling
  3. Adrenergic Receptor
  4. Bufuralol

Bufuralol  (Synonyms: Ro 3-4787)

Cat. No.: HY-105124 Purity: 99.17%
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Bufuralol (Ro 3-4787) is a potent non-selective, orally active β-adrenoreceptor antagonist with partial agonist activity. Bufuralol hydrochloride is a CYP2D6 probe substrate.

For research use only. We do not sell to patients.

Bufuralol Chemical Structure

Bufuralol Chemical Structure

CAS No. : 54340-62-4

Size Price Stock Quantity
1 mg USD 172 In-stock
5 mg USD 430 In-stock
10 mg USD 690 In-stock
25 mg USD 1500 In-stock
50 mg USD 2400 In-stock
100 mg USD 3850 In-stock
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Based on 1 publication(s) in Google Scholar

Other Forms of Bufuralol:

Bufuralol Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Bufuralol

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α adrenergic receptor β adrenergic receptor

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Bufuralol (Ro 3-4787) is a potent non-selective, orally active β-adrenoreceptor antagonist with partial agonist activity. Bufuralol hydrochloride is a CYP2D6 probe substrate[1][2][3][4].

IC50 & Target[1]

β-adrenoceptor

 

In Vitro

Bufuralol (Ro 3-4787) is widely used in the characterization of CYP2D6 activity, and possesses aromatic rings and a basic nitrogen that are characteristic of CYP2D6 substrates[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Bufuralol Related Antibodies
In Vivo

Bufuralol (Ro 3-4787) metabolism mediated by NADPH exhibits biphasic kinetics and is less efficient than that observed in the presence of cumene hydroperoxide (CuOOH) in and monkey intestines, in agreement with the observations in the livers[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

261.36

Formula

C16H23NO2
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

CCC1=CC=CC2=C1OC(C(O)CNC(C)(C)C)=C2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (382.61 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.8261 mL 19.1307 mL 38.2614 mL
5 mM 0.7652 mL 3.8261 mL 7.6523 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 3.5 mg/mL (13.39 mM); Clear solution

    This protocol yields a clear solution of ≥ 3.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (35.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 3.5 mg/mL (13.39 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 3.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (35.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.8261 mL 19.1307 mL 38.2614 mL 95.6535 mL
5 mM 0.7652 mL 3.8261 mL 7.6523 mL 19.1307 mL
10 mM 0.3826 mL 1.9131 mL 3.8261 mL 9.5654 mL
15 mM 0.2551 mL 1.2754 mL 2.5508 mL 6.3769 mL
20 mM 0.1913 mL 0.9565 mL 1.9131 mL 4.7827 mL
25 mM 0.1530 mL 0.7652 mL 1.5305 mL 3.8261 mL
30 mM 0.1275 mL 0.6377 mL 1.2754 mL 3.1885 mL
40 mM 0.0957 mL 0.4783 mL 0.9565 mL 2.3913 mL
50 mM 0.0765 mL 0.3826 mL 0.7652 mL 1.9131 mL
60 mM 0.0638 mL 0.3188 mL 0.6377 mL 1.5942 mL
80 mM 0.0478 mL 0.2391 mL 0.4783 mL 1.1957 mL
100 mM 0.0383 mL 0.1913 mL 0.3826 mL 0.9565 mL
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Bufuralol Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Bufuralol54340-62-4Ro 3-4787Adrenergic ReceptorBeta ReceptorCYP2D6probesubstratenon-selectiveorallyβ-adrenoreceptorInhibitorinhibitorinhibit

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