Etamicastat hydrochloride (BIA 5-453 hydrochloride) is a potent and reversible dopamine-β-hydroxylase ( DBH ) inhibitor with an IC 50 value of 107 nM. Etamicastat can be used in the research of cardiovascular diseases.
Storage Temp
Store at 2-8°C
Shipped In
Wet ice
Product Description
Etamicastat hydrochloride (BIA 5-453 hydrochloride) is a potent and reversible dopamine-β-hydroxylase ( DBH ) inhibitor with an IC 50 value of 107 nM Etamicastat can be used in the research of cardiovascular diseases .
In Vitro
Etamicastat blocks the hERG current amplitude with an IC 50 value of 44 μg/mL (141 μM). MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Etamicastat (100 mg/kg; administered intraperitoneally) leads to a significant reduction of noradrenaline levels in heart with concomitant increasing in dopamine levels . Etamicastat (50 mg/kg; a single oral administration) exhibits moderate oral bioavailability (64%), C max (4.9 nM), and terminal elimination half-lives (T 1/2 =3.7 h) in male Wistar rats . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: NMRi mice Dosage: 100 mg/kg Administration: Administered intraperitoneally Result: Led to a significant reduction of noradrenaline levels (36% control) in heart with concomitant increasing in dopamine levels (850% of control). Animal Model: Male Wistar rats Dosage: 50 mg/kg (Pharmacokinetic Analysis) Administration: Orally administered with at a dose volume of 10 mL/kg Result: Oral bioavailability (64%), C max (4.9 nM), and (T 1/2 =3.7 h).
