| Description | Etamicastat can be used in the research of cardiovascular diseases. Etamicastat (BIA 5-453) is a potent and reversible dopamine-β-hydroxylase (DBH) inhibitor with an IC50 value of 107 nM. |
| In vitro | Etamicastat blocks the hERG current amplitude with an IC50 value of 44 μg/mL. |
| In vivo | Etamicastat (50 mg/kg;?a single oral administration) exhibits moderate oral bioavailability (64%), Cmax (4.9 nM), and terminal elimination half-lives (T1/2=3.7 h) in male Wistar rats.Etamicastat (100 mg/kg; administered intraperitoneally) leads to a significant reduction of noradrenaline levels in heart with concomitant increasing in dopamine levels. |
| Target activity | DBH:107 nM |
| Synonyms | BIA 5-453 |
| molecular weight | 311.35 |
| Molecular formula | C14H15F2N3OS |
| CAS | 760173-05-5 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| References | 1. Loureiro AI, et al. Etamicastat, a new dopamine-ß-hydroxylase inhibitor, pharmacodynamics and metabolism in rat. Eur J Pharmacol. 2014 Oct 5;740:285-94. 2. ManuelVaz-da-Silva, et al. Cardiac safety profile of etamicastat, a novel peripheral selective dopamine-β-hydroxylase inhibitor in non-human primates, human young and elderly healthy volunteers and hypertensive patients. IJC Metabolic & Endocrine. 2015 Jun; (7): 10-24 |