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

Zamicastat (Synonyms: BIA 5-1058)

Cat. No.: HY-106004 Purity: 99.95% ee.: 99.43%
Handling Instructions

Zamicastat (BIA 5-1058) is a dopamine β-hydroxylase (DBH) inhibitor that could cross the blood-brain barrier (BBB) and 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. 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

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 275 In-stock
Estimated Time of Arrival: December 31
5 mg USD 250 In-stock
Estimated Time of Arrival: December 31
10 mg USD 450 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1350 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2100 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
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Description

Zamicastat (BIA 5-1058) is a dopamine β-hydroxylase (DBH) inhibitor that could cross the blood-brain barrier (BBB) and 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]. 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].

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].

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
Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 150 mg/mL (373.63 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

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
10 mM 0.2491 mL 1.2454 mL 2.4908 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.23 mM); Clear solution

  • 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

  • 3.

    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

*All of the co-solvents are provided by MCE.
References
Molecular Weight

401.47

Formula

C₂₁H₂₁F₂N₃OS

CAS No.

1080028-80-3

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere

Purity: 99.95% ee.: 99.43%

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Product Name:
Zamicastat
Cat. No.:
HY-106004
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Zamicastat

Cat. No.: HY-106004