Zamicastat

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].

Product Specifications

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.