Etamicastat (hydrochloride)


CAS No. : 677773-32-9

(Synonyms: BIA 5-453 (hydrochloride))

677773-32-9
Price and Availability of CAS No. : 677773-32-9
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5mg $390 In-stock
10mg $580 In-stock
50mg $1300 In-stock
100mg $1850 In-stock
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Cat. No. : HY-14838A
M.Wt: 347.81
Formula: C14H16ClF2N3OS
Purity: >98 %
Solubility: DMSO : 100 mg/mL (ultrasonic);H2O : 16.67 mg/mL (ultrasonic)
Introduction of 677773-32-9 :

Etamicastat hydrochloride (BIA 5-453 hydrochloride) 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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