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Zamicastat

Catalog No. T13383 CAS 1080028-80-3

Synonyms: BIA 5-1058

Zamicastat 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

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Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Zamicastat 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	Dopamine β-hydroxylase:, P-gp:73.8 μM , BCRP:17.0 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 2 years

Solubility Information

DMSO: 150 mg/mL (373.63 mM), Need ultrasonic

( < 1 mg/ml refers to the product slightly soluble or insoluble )

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.

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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.

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Tech Support

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 代谢离子通道神经科学 BCRP Hydroxylase P-gp ABCB1 Dopamine β-monooxygenase Inhibitor Cluster of differentiation 243 ABCG2 inhibit P-glycoprotein BIA 5-1058 Multidrug resistance protein 1 MDR1 CD243 Breast cancer resistance protein Pgp Dopamine β-hydroxylase Dopamine beta-hydroxylase Dopamine beta-monooxygenase inhibitor

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