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Zamicastat

  Cat. No.:  DC39048   Featured
Chemical Structure
1080028-80-3
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More than 5000 active chemicals with high quality for research!
Field of application
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 7
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 1080028-80-3
SMILES: C1C2C=C(F)C=C(F)C=2OC[C@@H]1N1C(=S)NC=C1CCNCC1C=CC=CC=1
Formula: C21H21F2N3Os
M.Wt: 401.473
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
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.
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.
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