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Cat. No.: HY-14838

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Etamicastat

(Synonyms: BIA 5-453)

Etamicastat (BIA 5-453) is a potent and reversible dopamine-β-hydroxylase (DBH) inhibitor with an IC₅₀ value of 107 nM. Etamicastat can be used in the research of cardiovascular diseases.

For research use only. We do not sell to patients.

CAS No.: 760173-05-5
Formula: C₁₄H₁₅F₂N₃OS
Molecular Weight:311.35

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (274 KB)

Etamicastat Chemical Structure

CAS No.: 760173-05-5

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
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Bioz

Biological Activity

Description

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].

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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).

Chemical Information

CAS No. 760173-05-5
Molecular Weight 311.35
Formula C₁₄H₁₅F₂N₃OS
SMILES

S=C1NC=C(CCN)N1[C@H]2COC3=C(C=C(F)C=C3F)C2
Synonyms

BIA 5-453
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (274 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Loureiro AI, et al. Etamicastat, a new dopamine-ß-hydroxylase inhibitor, pharmacodynamics and metabolism in rat. Eur J Pharmacol. 2014 Oct 5;740:285-94. [Content Brief]

[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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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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