(R)-5-(2-Aminoethyl)-1-(6,8-difluorochroman-3-yl)-1,3-dihydroimidazole-2-thione

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Products Intro: Product Name:(r)-5-(2-aminoethyl)-1-(6,8-difluorochroman-3-yl)-1,3-dihydroimidazole-2-thione
CAS:760173-05-5
Purity:0.99 Package:1kg
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Products Intro: Product Name:Etamicastat；BIA 5-453
CAS:760173-05-5
Purity:98.00% Package:100 mg；500 mg Remarks:REAGENT;FOR LABORATORY USE ONLY
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Products Intro: Product Name:Etamicastat
CAS:760173-05-5
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Products Intro: Product Name:Etamicastat
CAS:760173-05-5
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Products Intro: Product Name:Etamicastat
CAS:760173-05-5
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(R)-5-(2-Aminoethyl)-1-(6,8-difluorochroman-3-yl)-1,3-dihydroimidazole-2-thione manufacturers

  • Etamicastat
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  • $2420.00
  • 2026-05-11
  • CAS:760173-05-5
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  • Supply Ability: 10g
  • Etamicastat
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  • $2420.00
  • 2025-07-18
  • CAS:760173-05-5
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  • Supply Ability: 10g
(R)-5-(2-Aminoethyl)-1-(6,8-difluorochroman-3-yl)-1,3-dihydroimidazole-2-thione Basic information
Product Name:(R)-5-(2-Aminoethyl)-1-(6,8-difluorochroman-3-yl)-1,3-dihydroimidazole-2-thione
Synonyms:(R)-5-(2-Aminoethyl)-1-(6,8-difluorochroman-3-yl)-1,3-dihydroimidazole-2-thione;BIA 5-453;2H-Imidazole-2-thione, 5-(2-aminoethyl)-1-[(3R)-6,8-difluoro-3,4-dihydro-2H-1-benzopyran-3-yl]-1,3-dihydro-;EtaMicastat
CAS:760173-05-5
MF:C14H15F2N3OS
MW:311.35
EINECS:
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Mol File:760173-05-5.mol
(R)-5-(2-Aminoethyl)-1-(6,8-difluorochroman-3-yl)-1,3-dihydroimidazole-2-thione Structure
(R)-5-(2-Aminoethyl)-1-(6,8-difluorochroman-3-yl)-1,3-dihydroimidazole-2-thione Chemical Properties
Boiling point 435.3±55.0 °C(Predicted)
density 1.44
storage temp. Store at -20°C
solubility Soluble in DMSO
pka11.73±0.70(Predicted)
form powder
color white to beige
Safety Information
WGK Germany WGK 3
Storage Class11 - Combustible Solids
MSDS Information
(R)-5-(2-Aminoethyl)-1-(6,8-difluorochroman-3-yl)-1,3-dihydroimidazole-2-thione Usage And Synthesis
UsesEtamicastat (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 ActivityOrally active, potent, reversible and peripherally selective dopamine-β-hydroxylase (DBH) inhibitor.
Etamicast at (BIA 5-453) is an orally active, potent, reversible 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).
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
(R)-5-(2-Aminoethyl)-1-(6,8-difluorochroman-3-yl)-1,3-dihydroimidazole-2-thione Preparation Products And Raw materials
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