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

Etamicastat hydrochloride (Synonyms: BIA 5-453 hydrochloride)

Cat. No.: HY-14838A
Handling Instructions

Etamicastat hydrochloride (BIA 5-453 hydrochloride) 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.

Etamicastat hydrochloride Chemical Structure

Etamicastat hydrochloride Chemical Structure

CAS No. : 677773-32-9

Size Stock
100 mg   Get quote  
250 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Other Forms of Etamicastat hydrochloride:

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Etamicastat hydrochloride (BIA 5-453 hydrochloride) 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].

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).
Molecular Weight

347.81

Formula

C₁₄H₁₆ClF₂N₃OS

CAS No.

677773-32-9

SMILES

FC1=CC(F)=C2OC[[email protected]@H](CC2=C1)N3C(CCN)=CNC3=S.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
= × ×

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

Keywords:

EtamicastatBIA 5-453Dopamine β-hydroxylaseDopamine beta-hydroxylaseDopamine beta-monooxygenaseDopamine β-monooxygenaseCardiacriskDBHcardiovasculardiseasesInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product name

 

Salutation

Applicant name *

 

Email address *

Phone number *

 

Organization name *

Country or Region *

 

Requested quantity *

Remarks

Bulk Inquiry

Inquiry Information

Product name:
Etamicastat hydrochloride
Cat. No.:
HY-14838A
Quantity:
MCE Japan Authorized Agent: