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

Etamicastat hydrochloride  (Synonyms: BIA 5-453 hydrochloride)

Cat. No.: HY-14838A Purity: 98.14%
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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 Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 429 In-stock
Solution
10 mM * 1 mL in DMSO USD 429 In-stock
Solid
5 mg USD 390 In-stock
10 mg USD 580 In-stock
50 mg USD 1300 In-stock
100 mg USD 1850 In-stock
200 mg   Get quote  
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Based on 1 publication(s) in Google Scholar

Other Forms of Etamicastat hydrochloride:

Etamicastat hydrochloride Related Antibodies

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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].

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

Etamicastat hydrochloride 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

347.81

Formula

C14H16ClF2N3OS
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (287.51 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 16.67 mg/mL (47.93 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8751 mL 14.3757 mL 28.7513 mL
5 mM 0.5750 mL 2.8751 mL 5.7503 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (7.19 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (7.19 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 2.8751 mL 14.3757 mL 28.7513 mL 71.8783 mL
5 mM 0.5750 mL 2.8751 mL 5.7503 mL 14.3757 mL
10 mM 0.2875 mL 1.4376 mL 2.8751 mL 7.1878 mL
15 mM 0.1917 mL 0.9584 mL 1.9168 mL 4.7919 mL
20 mM 0.1438 mL 0.7188 mL 1.4376 mL 3.5939 mL
25 mM 0.1150 mL 0.5750 mL 1.1501 mL 2.8751 mL
30 mM 0.0958 mL 0.4792 mL 0.9584 mL 2.3959 mL
40 mM 0.0719 mL 0.3594 mL 0.7188 mL 1.7970 mL
DMSO 50 mM 0.0575 mL 0.2875 mL 0.5750 mL 1.4376 mL
60 mM 0.0479 mL 0.2396 mL 0.4792 mL 1.1980 mL
80 mM 0.0359 mL 0.1797 mL 0.3594 mL 0.8985 mL
100 mM 0.0288 mL 0.1438 mL 0.2875 mL 0.7188 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Etamicastat hydrochloride Related Classifications

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  • 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:

Etamicastat677773-32-9BIA 5-453Dopamine β-hydroxylaseDopamine beta-hydroxylaseDopamine beta-monooxygenaseDopamine β-monooxygenaseCardiacriskDBHcardiovasculardiseasesInhibitorinhibitorinhibit

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