| Identification | Back Directory | [Name]
(R)-5-(2-Aminoethyl)-1-(6,8-difluorochroman-3-yl)-1,3-dihydroimidazole-2-thione | [CAS]
760173-05-5 | [Synonyms]
BIA 5-453
EtaMicastat
(R)-5-(2-Aminoethyl)-1-(6,8-difluorochroman-3-yl)-1,3-dihydroimidazole-2-thione | [Molecular Formula]
C14H15F2N3OS | [MDL Number]
MFCD16619338 | [MOL File]
760173-05-5.mol | [Molecular Weight]
311.35 |
| Chemical Properties | Back Directory | [Boiling point ]
435.3±55.0 °C(Predicted) | [density ]
1.44 | [storage temp. ]
Store at -20°C | [solubility ]
Soluble in DMSO | [form ]
powder | [pka]
11.73±0.70(Predicted) | [color ]
white to beige |
| Hazard Information | Back Directory | [Uses]
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]. | [Biological Activity]
Orally activepotentreversible and peripherally selective dopamine-β-hydroxylase (DBH) inhibitor.
Etamicast at (BIA 5-453) is an orally activepotentreversible and peripherally selective dopamine-β-hydroxylase (DBH) inhibitor th at reduces both systolic (SBP) and diastolic (DBP) blood pressure. | [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].
| Animal Model: | NMRi mice[1] | | 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[1] | | Dosage: | 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). |
| [storage]
Store at -20°C | [References]
[1] Loureiro AI, et al. Etamicastat, a new dopamine-?-hydroxylase inhibitor, pharmacodynamics and metabolism in rat. Eur J Pharmacol. 2014 Oct 5;740:285-94. DOI:10.1016/j.ejphar.2014.07.027
[2] ManuelVaz-da-Silva, et al. Cardiac safety profile of etamicastat, a novel peripheral selective dopamine-β-hydroxylase inhibitor in non-human primates, human young and elderly healthy volunteers and hypertensive patients. IJC Metabolic & Endocrine. 2015 Ju |
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