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Zamicastat

CAT: 0804-HY-106004-01Size: 5 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-106004-01Size:5 mg
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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].
CAS Number
1080028-80-3
Product Name Alternative
BIA 5-1058
UNSPSC
12352005
Target
BCRP; Dopamine β-hydroxylase; P-glycoprotein
Type
Reference compound
Related Pathways
Membrane Transporter/Ion Channel; Metabolic Enzyme/Protease
Applications
Cancer-programmed cell death
Field of Research
Cancer; Cardiovascular Disease
Assay Protocol
https://www.medchemexpress.com/Zamicastat.html
Concentration
10mM
Purity
99.95
Solubility
DMSO : 150 mg/mL (ultrasonic)
Smiles
S=C1N([C@@H]2CC3=CC(F)=CC(F)=C3OC2)C(CCNCC4=CC=CC=C4)=CN1
Molecular Formula
C21H21F2N3OS
Molecular Weight
401.47
References & Citations
[1]Bicker J, et al. In vitro assessment of the interactions of dopamine β-hydroxylase inhibitors with human P-glycoprotein and Breast Cancer Resistance Protein. Eur J Pharm Sci. 2018 May 30;117:35-40.|[2]Igreja B, et al. Effects of Zamicastat treatment in a genetic model of salt-sensitive hypertension and heart failure. Eur J Pharmacol. 2019 Jan 5;842:125-132.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
Phase 2