Etamicastat
CAS No. : 760173-05-5
(Synonyms: BIA 5-453)
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| Cat. No. : | HY-14838 |
| M.Wt: | 311.35 |
| Formula: | C14H15F2N3OS |
| Purity: | >98 % |
| Solubility: | 10 mM in DMSO |
Etamicastat (BIA 5-453) is a potent and reversible dopamine-β-hydroxylase (DBH) inhibitor with an IC50 value of 107 nM[1]. Etamicastat can be used in the research of cardiovascular diseases[2].
IC50 & Target: IC50: 107 nM (DBH)[1]
In Vitro: Etamicastat blocks the hERG current amplitude with an IC50 value of 44 μg/mL (141 μM)[2].
In Vivo: Etamicastat (100 mg/kg; administered intraperitoneally) leads to a significant reduction of noradrenaline levels in heart with concomitant increasing in dopamine levels[1].
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[1].
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