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Zamicastat

Name: Zamicastat
Brand: TargetMol
SKU: T13383
Price: 88 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T13383Cas No. 1080028-80-3

Alias BIA 5-1058

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

Zamicastat

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Purity: 99.58%

Catalog No. T13383Alias BIA 5-1058Cas No. 1080028-80-3

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

Pack Size	Price	Availability
1 mg	$88	In Stock
5 mg	$215	In Stock
10 mg	$325	In Stock
25 mg	$587	In Stock
50 mg	$883	In Stock
100 mg	$1,280	In Stock
1 mL x 10 mM (in DMSO)	$233	In Stock

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Purity:99.58%

ee:100%

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Product Introduction

Bioactivity

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

Chemical Properties

Molecular Weight	401.47
Formula	C₂₁H₂₁F₂N₃OS
Cas No.	1080028-80-3
Smiles	Fc1cc(F)c2OC[C@@H](Cc2c1)n1c(CCNCc2ccccc2)c[nH]c1=S
Relative Density.	1.36 g/cm3 (Predicted)
Color	White
Appearance	Solid

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

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

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 4 mg/mL (9.96 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.4908 mL	12.4542 mL	24.9085 mL	124.5423 mL
5 mM	0.4982 mL	2.4908 mL	4.9817 mL	24.9085 mL
10 mM	0.2491 mL	1.2454 mL	2.4908 mL	12.4542 mL
20 mM	0.1245 mL	0.6227 mL	1.2454 mL	6.2271 mL
50 mM	0.0498 mL	0.2491 mL	0.4982 mL	2.4908 mL
100 mM	0.0249 mL	0.1245 mL	0.2491 mL	1.2454 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:

For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments

A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent

DMSO+30% PEG300+5% Tween 80+60% Saline/PBS/ddH₂O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.

Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH₂O TargetMol | reagent

mix well and clarify

For Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.

All types of co-solvents required for the protocol, such asDMSO, PEG300/ PEG400, Tween 80, SBE-β-CD, corn oil are available for purchase on the TargetMol website with a simple click.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Sci Citations

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