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Merck
CN

SML3857

Sigma-Aldrich

Etamicastat

≥98% (HPLC)

Synonym(s):

(R)-5-(2-Aminoethyl)-1-(6,8-difluorochroman-3-yl)-1,3-dihydroimidazole-2-thione, (R)-5-(2-Aminoethyl)-1-(6,8-difluorochroman-3-yl)-1H-imidazole-2(3H)-thione, 5-​(2-​Aminoethyl)​-​1-​[(3R)​-​6,​8-​difluoro-​3,​4-​dihydro-​2H-​1-​benzopyran-​3-​yl]​-​1,​3-​dihydro-2H-iImidazole-​2-​thione, BIA 5-453

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About This Item

Empirical Formula (Hill Notation):
C14H15F2N3OS
CAS Number:
Molecular Weight:
311.35
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
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Quality Level

Assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

-10 to -25°C

Biochem/physiol Actions

Orally active, potent, reversible and peripherally selective dopamine-β-hydroxylase (DBH) inhibitor.
Etamicastat (BIA 5-453) is an orally active, potent, reversible and peripherally selective dopamine-β-hydroxylase (DBH) inhibitor that reduces both systolic (SBP) and diastolic (DBP) blood pressure.

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Regulatory Information

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Dopamine ? hydroxylase as a potential drug target to combat hypertension
Expert Opinion on Investigational Drugs, 29(9), 1043-1057 (2020)
Effect of food on the pharmacokinetic profile of etamicastat (BIA 5-453)
Drugs in R&D, 11(2), 127-136 (2011)
Characterization of the interaction of the novel antihypertensive etamicastat with human dopamine-?-hydroxylase: comparison with nepicastat
European Journal of Pharmacology, 751, 50-58 (2015)

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