2. Metabolic Enzyme/Protease
  3. Dopamine β-hydroxylase
  4. Etamicastat

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.

At equivalent molar concentrations, both the salt and free forms of a compound exhibit comparable biological activity. Nevertheless, the salt form (Etamicastat hydrochloride) usually boasts enhanced water solubility and stability.

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

Etamicastat Chemical Structure

Etamicastat Chemical Structure

CAS No. : 760173-05-5

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Etamicastat Related Antibodies

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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.

Etamicastat Related Antibodies
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].

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%), Cmax (4.9 nM), and (T1/2=3.7 h).
Molecular Weight

311.35

Formula

C14H15F2N3OS
CAS No.
SMILES

S=C1NC=C(CCN)N1[C@H]2COC3=C(C=C(F)C=C3F)C2
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
References
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Etamicastat Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Etamicastat760173-05-5BIA 5-453Dopamine β-hydroxylaseDopamine beta-hydroxylaseDopamine beta-monooxygenaseDopamine β-monooxygenaseCardiacriskDBHcardiovasculardiseasesInhibitorinhibitorinhibit

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