ChemicalBook CAS DataBase List 760173-05-5

760173-05-5

Name	(R)-5-(2-Aminoethyl)-1-(6,8-difluorochroman-3-yl)-1,3-dihydroimidazole-2-thione
CAS	760173-05-5
Molecular Formula	C14H15F2N3OS
MDL Number	MFCD16619338
Molecular Weight	311.35
MOL File	760173-05-5.mol

Chemical Properties

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

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%), C_max (4.9 nM), and terminal elimination half-lives (T_1/2=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%), C_max (4.9 nM), and (T_1/2=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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