Acebutolol HCl

Catalog No.S4010

For research use only.

Acebutolol is a β-adrenergic receptors antagonist used in the treatment of hypertension, angina pectoris and cardiac arrhythmias.

Acebutolol HCl Chemical Structure

CAS No. 34381-68-5

Selleck's Acebutolol HCl has been cited by 1 Publication

Purity & Quality Control

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Biological Activity

Description Acebutolol is a β-adrenergic receptors antagonist used in the treatment of hypertension, angina pectoris and cardiac arrhythmias.
Features Acebutolol has stabilizing and quinidine-like effects on cardiac rhythm as well as weak inherent sympathomimetic action.
Targets
β-adrenergic receptor [1]
In vitro

Acebutolol inhibits NA uptake in rat brain P2 fractions with IC50 of 0.25 mM. [1] Acebutolol produces a concentration-dependent inhibition of 125I-labeled CYP binding to human fat cell membranes and are able to completely displace all specifically bound radioligand. Acebutolol totally inhibits lipolytic activity initiated by 1 μM isoproterenol. Acebutolol is a cardioselective antagonist possessing low lipid solubility. [2] Acebutolol, which does not bind to LDL, shows a stronger inhibiting effect on the intracellular accumulation of cholesterol esters in J774 macrophages than alprenolol and oxprenolol which bind to LDL. [3]

In vivo Acebutolol following single intravenous administration (10 mg/kg) to rat results in the plasma clearance of 61.9 mL/min/kg, the volume of distribution of 9.6 L/kg, and an elimination half-life of 1.8 hours. Acebutolol following single intravenous administration (50 mg/kg) to rat results in the plasma clearance of 46.5 mL/min/kg, the volume of distribution of 9.5 L/kg, and an elimination half-life of 2.3 hours. [4] Acebutolol (30 mg/kg) decreases cardiac output by 65% and 31% after 1 min and 10 min measurements, respectively, in Sprague-Dawley rats. Acebutolol (30 mg/kg) significantly reduces regional blood flow (RBF) in most organs either after 1 min or 10 min measurements when compare with the baseline values in Sprague-Dawley rats. [5]

Protocol (from reference)

Animal Research:[4]
  • Animal Models: Sprague–Dawley rats
  • Dosages: 10 mg/kg
  • Administration: Intravenously
  • (Only for Reference)

Solubility (25°C)

In vitro

DMSO 75 mg/mL
(201.13 mM)
Water 75 mg/mL
(201.13 mM)
Ethanol 75 mg/mL
(201.13 mM)

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
Saline
For best results, use promptly after mixing.

30 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 372.89
Formula

C18H28N2O4.HCl

 
CAS No. 34381-68-5
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CCCC(=O)NC1=CC(=C(C=C1)OCC(CNC(C)C)O)C(=O)C.Cl

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT01514019 Completed Drug: Acebutolol|Drug: Placebo Healthy In-Jin Jang MD PhD|Oita University|Seoul National University Hospital|Kyushu University January 2012 Phase 4

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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