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Zamicastat

Catalog No. T13383 CAS 1080028-80-3

Synonyms: BIA 5-1058

Zamicastat (BIA 5-1058) is an inhibitor of dopamine β-hydroxylase (DBH), and is also a concentration-dependent dual inhibitor of P-gp and BCRP(IC50 values of 73.8 μM and 17.0 μM, respectively).

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Zamicastat, CAS 1080028-80-3

Pack Size	Availability	Price/USD
1 mg	In stock	$ 101.00
5 mg	In stock	$ 223.00
10 mg	In stock	$ 397.00
25 mg	In stock	$ 665.00
50 mg	In stock	$ 947.00
100 mg	In stock	$ 1,280.00
1 mL * 10 mM (in DMSO)	In stock	$ 233.00

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Purity: 97.43%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Zamicastat (BIA 5-1058) is an inhibitor of dopamine β-hydroxylase (DBH), and is also a concentration-dependent dual inhibitor of P-gp and BCRP(IC50 values of 73.8 μM and 17.0 μM, respectively).
Targets&IC50	BCRP:17.0 μM , Dopamine β-hydroxylase:, P-gp:73.8 μM
In vivo	In the Dahl SS rat, Zamicastat (10, 30 and 100 mg/kg/day; oral bolus, 7 days) is tested acutely against salt-induced hypertension. Zamicastat produces a dose-dependent decrease in blood pressure[2].

Synonyms	BIA 5-1058
Molecular Weight	401.47
Formula	C21H21F2N3OS
CAS No.	1080028-80-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 150 mg/mL (373.63 mM), Sonification is recommended.

References and Literature

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.

Related compound libraries

This product is contained In the following compound libraries：

Drug Repurposing Compound Library Anti-Cancer Clinical Compound Library Anti-Cancer Drug Library Inhibitor Library Bioactive Compounds Library Max NO PAINS Compound Library Bioactive Compound Library Anti-Hypertension Compound Library Metabolism Compound Library Ion Channel Inhibitor Library

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Related compounds with same targets

GS-9191 PM Elacridar YHO-13177 Ko 143 Brevianamide F ABCG2-IN-2 PCI 29732 ABCG2-IN-1

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Zamicastat 1080028-80-3 Membrane transporter/Ion channel Metabolism Neuroscience P-gp Hydroxylase BCRP ABCB1 Dopamine β-monooxygenase Inhibitor Cluster of differentiation 243 ABCG2 inhibit P-glycoprotein Multidrug resistance protein 1 BIA 5-1058 MDR1 CD243 Breast cancer resistance protein Pgp Dopamine β-hydroxylase Dopamine beta-hydroxylase Dopamine beta-monooxygenase inhibitor

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