Etamicastat hydrochloride

Research use only, not for human use.

Etamicastat hydrochloride (BIA 5-453 hydrochloride) is a peripherally selective dopamine beta-hydroxylase inhibitor that reduces hypertension.

Etamicastat hydrochloride (BIA 5-453 hydrochloride) is a potent and reversible dopamine-β-hydroxylase (DBH) inhibitor with an IC50 value of 107 nM. Etamicastat can be used in the research of cardiovascular diseases.

Etamicastat blocks the hERG current amplitude with an IC50 value of 44 μg/mL (141 μM).

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%), Cmax (4.9 nM), and terminal elimination half-lives (T1/2=3.7 h) in male Wistar rats.Animal Model:NMRi mice Dosage:100 mg/kg Administration:Administered intraperitoneallyResult: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 ratsDosage:50 mg/kg (Pharmacokinetic Analysis) Administration:Orally administered with at a dose volume of 10 mL/kg Result:Oral bioavailability (64%), Cmax (4.9 nM), and (T1/2=3.7 h).

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Metabolic Enzyme/Protease

Dehydrogenase

Dehydrogenase

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677773-32-9

347.81

C14H16ClF2N3OS

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (287.51 mM; Ultrasonic ) H2O : 16.67 mg/mL (47.93 mM; Ultrasonic)

Cl.NCCc1c[nH]c(=S)n1[C@H]1COc2c(F)cc(F)cc2C1

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(-20℃)

With Ice Pack

≥ 2 years