Acebutolol HCl (C09-0734-702)

InformationAcebutolol is aβ-adrenergic receptorsantagonist used in the treatment of hypertension, angina pectoris and cardiac arrhythmias.In vitroAcebutolol inhibits NA uptake in rat brain P2 fractions with IC50 of 0.25 mM. 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. 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.In vivoAcebutolol following single intravenous administration (10 mg/kg) to rat results in the plasma clearance of 61.9/u2009mL/min/kg, the volume of distribution of 9.6/u2009L/kg, and an elimination half-life of 1.8/u2009hours. Acebutolol following single intravenous administration (50 mg/kg) to rat results in the plasma clearance of 46.5/u2009mL/min/kg, the volume of distribution of 9.5/u2009L/kg, and an elimination half-life of 2.3/u2009hours. 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.Cell Datacell lines：RS4;11, MV4;11, and OC1-AML5Concentrations：Incubation Time：Powder Purity:≥99%. Specification: 10mM in DMSO Molecular Formula: C18H28N2O4·HCl  Molecular Weight: 372.89