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.

Etamicastat blocks the hERG current amplitude with an IC50 value of 44 μg/mL.

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.

760173-05-5

C14H15F2N3OS

311.35

BIA 5-453

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years