1080028-80-3

1080028-80-3 structure

Name: Zamicastat
Chemical Name: 4-[2-(benzylamino)ethyl]-3-[(3R)-6,8-difluoro-3,4-dihydro-2H-chromen-3-yl]-1H-imidazole-2-thione
CAS Number: 1080028-80-3
Molecular Formula: C₂₁H₂₁F₂N₃OS
Molecular Weight: 401.47300
Catalog: Signaling Pathways Membrane Transporter/Ion Channel BCRP
Create Date: 2016-01-28 14:54:02
Modify Date: 2024-01-09 19:45:35
Zamicastat is a concentration-dependent dual P-gp and BCRP inhibitor with IC50 values of 73.8±7.2 μM and 17.0±2.7 μM, respectively.

Name	4-[2-(benzylamino)ethyl]-3-[(3R)-6,8-difluoro-3,4-dihydro-2H-chromen-3-yl]-1H-imidazole-2-thione
Synonyms	Zamitat UNII-YLU32D0DNV

Description	Zamicastat is a concentration-dependent dual P-gp and BCRP inhibitor with IC50 values of 73.8±7.2 μM and 17.0±2.7 μM, respectively.
Related Catalog	Signaling Pathways >> Membrane Transporter/Ion Channel >> BCRP Signaling Pathways >> Membrane Transporter/Ion Channel >> P-glycoprotein Research Areas >> Cancer
Target	IC50: 73.8±7.2 μM (P-gp), 17.0±2.7 μM (BCRP)[1]
In Vitro	Zamicastat is a concentration-dependent dual P-glycoprotein (P-gp) and breast cancer resistance protein (BCRP) inhibitor with IC50 values of 73.8±7.2 μM and 17.0±2.7 μM. Zamicastat also reversibly inhibits dopamine β-hydroxylase (DBH) without effect in brain tissue[1].
References	[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.