2. Metabolic Enzyme/Protease Membrane Transporter/Ion Channel
  3. Dopamine β-hydroxylase P-glycoprotein BCRP
  4. Zamicastat

Zamicastat  (Synonyms: BIA 5-1058)

Cat. No.: HY-106004 Purity: ≥98.0%
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Zamicastat (BIA 5-1058) est un inhibiteur de la dopamine β-hydroxylase (DBH) et peut traverser la barrière hémato-encéphalique (BHE) pour provoquer des effets centraux et périphériques. Zamicastat est également un double inhibiteur de P-gp et de BCRP concentration-dépendant avec des valeurs IC50 de 73,8 μM et 17,0 μM, respectivement. Zamicastat réduit l’hypertension.

Zamicastat (BIA 5-1058) is a dopamine β-hydroxylase (DBH) inhibitor and can cross the blood-brain barrier (BBB) to cause central as well as peripheral effects. Zamicastat is also a concentration-dependent dual P-gp and BCRP inhibitor with IC50 values of 73.8 μM and 17.0 μM, respectively. Zamicastat reduces high blood pressure.

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

Zamicastat Chemical Structure

Zamicastat Chemical Structure

CAS No. : 1080028-80-3

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
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Solution
10 mM * 1 mL in DMSO USD 288 In-stock
Solid
5 mg USD 262 In-stock
10 mg USD 394 In-stock
25 mg USD 710 In-stock
50 mg USD 1066 In-stock
100 mg USD 1600 In-stock
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Based on 1 publication(s) in Google Scholar

Zamicastat Related Antibodies

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Description

Zamicastat (BIA 5-1058) is a dopamine β-hydroxylase (DBH) inhibitor and can cross the blood-brain barrier (BBB) to cause central as well as peripheral effects. Zamicastat is also a concentration-dependent dual P-gp and BCRP inhibitor with IC50 values of 73.8 μM and 17.0 μM, respectively[1]. Zamicastat reduces high blood pressure[2].

IC50 & Target

Dopamine β-hydroxylase (DBH)[1]
IC50: 73.8 μM (P-gp), 17.0 μM (BCRP)[1]
In Vitro

Following 4 hours of incubation (5, 10, 20, 50, 80, 100 μM), a significant loss of cell viability is verified with 100 μM Zamicastat (p=0.010) in MDCK-BCRP cells. No significant losses of cell viability are observed after 4 h of incubation for other concentrations in all cell lines. By decreasing the incubation period to 30 min, there is no significant loss of cell viability (p>0.05) at 100 μM in all cell lines[1].

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

Zamicastat Related Antibodies

Cell Viability Assay[1]

Cell Line: MDCK II, MDCK-MDR1 and MDCK-BCRP cells
Concentration: 5, 10, 20, 50, 80, 100 μΜ
Incubation Time: 4 hours (5, 10, 20, 50, 80, 100 μM) or 30 min (only 100 μM)
Result: A significant loss of cell viability was verified with 100 μM in MDCK-BCRP cells.
In Vivo

Zamicastat (10, 30 and 100 mg/kg/day; oral bolus, 7 days) is tested acutely against salt-induced hypertension in the Dahl SS rat. Zamicastat produces a dose-dependent decrease in blood pressure. 24 h after Zamicastat administration mean systolic blood pressure (SBP) decrease is -12.6±4.1 mm Hg (P=0.0284), -15.2±2.7 mm Hg (P=0.0026) and -19.0±3.7 mm Hg (P=0.0036) for the 10, 30, and 100 mg/kg body weight dose, respectively. Zamicastat administration also produces a significant 24-h average decrease in diastolic blood pressure (DBP) of - 14.6±3.4 mm Hg (P=0.0073) with 10 mg/kg body weight dose, -13.0±4.5 mm Hg (P=0.0347) with 30 mg/kg body weight dose and -15.0±3.1 mm Hg (P=0.0046) with 100 mg/kg body weight dose. Zamicastat administration leads to a decrease in the 24h post-dose mean arterial pressure (MAP) of -13.4±3.8 mm Hg (P=0.0162), -14.0±3.5 mm Hg (P=0.0101) and -20.6±3.7 mm Hg (P=0.0026) for the 10, 30, and 100 mg/kg body weight dose, respectively. There is a small, but significant, effect of Zamicastat on the 24-h mean heart rate (HR) post-dose for all tested doses (10 mg/kg: -19.1±3.2 beats/min, P=0.0019; 30 mg/kg: -13.0±4.5 beats/min, P=0.0347; 100 mg/kg: -21.6±6.6 beats/min, P=0.0235)[2].

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

Animal Model: Six-week-old male inbred male Dahl SS rats[2]
Dosage: 10, 30, or 100 mg/kg; 4 mL/kg
Administration: Oral bolus, daily, seven days
Result: Treatment produced a dose-dependent decrease in blood pressure. Twenty four hours after administration mean SBP decrease was -12.6±4.1 mm Hg (P=0.0284), -15.2±2.7 mm Hg (P=0.0026) and -19.0±3.7 mm Hg (P=0.0036) for the 10, 30, and 100 mg/kg body weight dose, respectively.
Animal Model: ten-week-old male Wistar Han rats[2]
Dosage: 30 mg/kg/day
Administration: in animal feedings (mixed in meal rodent food) everyday
Result: lead to a significant 51% decrease in noradrenaline levels excreted in urine
Clinical Trial
Molecular Weight

401.47

Formula

C21H21F2N3OS
CAS No.
Appearance

Solid

Color

White to yellow

SMILES

S=C1N([C@@H]2CC3=CC(F)=CC(F)=C3OC2)C(CCNCC4=CC=CC=C4)=CN1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 150 mg/mL (373.63 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4908 mL 12.4542 mL 24.9085 mL
5 mM 0.4982 mL 2.4908 mL 4.9817 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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  • 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 (6.23 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 (6.23 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.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
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).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: ≥98.0%

COA (253 KB) HNMR (266 KB)

Handling Instructions (2659 KB)
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.4908 mL 12.4542 mL 24.9085 mL 62.2712 mL
5 mM 0.4982 mL 2.4908 mL 4.9817 mL 12.4542 mL
10 mM 0.2491 mL 1.2454 mL 2.4908 mL 6.2271 mL
15 mM 0.1661 mL 0.8303 mL 1.6606 mL 4.1514 mL
20 mM 0.1245 mL 0.6227 mL 1.2454 mL 3.1136 mL
25 mM 0.0996 mL 0.4982 mL 0.9963 mL 2.4908 mL
30 mM 0.0830 mL 0.4151 mL 0.8303 mL 2.0757 mL
40 mM 0.0623 mL 0.3114 mL 0.6227 mL 1.5568 mL
50 mM 0.0498 mL 0.2491 mL 0.4982 mL 1.2454 mL
60 mM 0.0415 mL 0.2076 mL 0.4151 mL 1.0379 mL
80 mM 0.0311 mL 0.1557 mL 0.3114 mL 0.7784 mL
100 mM 0.0249 mL 0.1245 mL 0.2491 mL 0.6227 mL
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Zamicastat Related Classifications

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:

Zamicastat1080028-80-3BIA 5-1058Dopamine β-hydroxylaseP-glycoproteinBCRPDopamine beta-hydroxylaseDopamine beta-monooxygenaseDopamine β-monooxygenaseP-gpPgpMultidrug resistance protein 1MDR1ATP-binding cassette sub-family B member 1ABCB1Cluster of differentiation 243CD243Breast cancer resistance proteinABCG2Inhibitorinhibitorinhibit

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