Antibodies
Acebutolol is a β-adrenergic receptors antagonist used in the treatment of hypertension, angina pectoris and cardiac arrhythmias.
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| Description | Acebutolol is a β-adrenergic receptors antagonist used in the treatment of hypertension, angina pectoris and cardiac arrhythmias. | |||||
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| Targets | β-adrenergic receptors | |||||
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| 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] | |||||
| Features | Acebutolol has stabilizing and quinidine-like effects on cardiac rhythm as well as weak inherent sympathomimetic action. | |||||
| Animal Models | Sprague–Dawley rats |
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| Dosages | 10 mg/kg |
| Administration | Intravenously |
| Solubility | Saline, 30 mg/mL |
| Molecular Weight (MW) | 372.89 |
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| Formula | C18H28N2O4.HCl |
| CAS No. | 34381-68-5 |
| Storage | 3 years -20℃Powder |
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| 6 months-80℃in DMSO | |
| Syonnyms | N/A |
| Solubility (25°C) * | In vitro | DMSO | 75 mg/mL (201 mM) |
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| Water | 75 mg/mL (201 mM) | ||
| Ethanol | 75 mg/mL (201 mM) | ||
| In vivo | Saline, | 30 mg/mL | |
| * <1 mg/ml means slightly soluble or insoluble. * 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 Name | Butanamide, N-[3-acetyl-4-[2-hydroxy-3-[(1-methylethyl)amino]propoxy]phenyl]-, hydrochloride (1:1) |
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| Stock Solution (1ml DMSO) | 1mM | 10mM | 20mM | 30mM |
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| Mass(mg) | 0.37289 | 3.7289 | 7.4578 | 11.1867 |