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Zileuton

Name: Zileuton
Brand: TargetMol
SKU: T0477
Price: 30 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T0477Cas No. 111406-87-2

Alias Abbott 64077, A 64077

Zileuton (A 64077) is a synthetic derivative of hydroxyurea with antiasthmatic properties. The leukotriene inhibitor zileuton blocks 5-lipoxygenase, which catalyzes the formation of leukotrienes from arachidonic acid; causes bronchodilation; decreases bronchial mucous secretion and edema; and may prevent or decrease the symptoms of asthma.

Zileuton

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Purity: 99.43%

Catalog No. T0477Alias Abbott 64077, A 64077Cas No. 111406-87-2

Pack Size	Price	USA Warehouse	Global Warehouse
10 mg	$30	In Stock	In Stock
25 mg	$44	In Stock	In Stock
50 mg	$61	In Stock	In Stock
100 mg	$87	In Stock	In Stock
200 mg	$127	In Stock	In Stock
500 mg	$209	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$50	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Purity:99.43%

Color:White

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Product Introduction

Zileuton AI Summary

Zileuton is a potent 5-lipoxygenase (5-LO) inhibitor with diverse bioactivities, demonstrating significant inhibition across various in vitro and in vivo assays. It effectively inhibits 5-LO-mediated conversion of arachidonic acid to inflammatory mediators like leukotriene B4 (LTB4) and 5-hydroxyeicosatetraenoic acid (5-HETE) in guinea pig leukocytes, human PMNLs, and human whole blood, with IC50 values ranging from 300 nM to 3700 nM. The compound also shows in vivo anti-inflammatory properties by inhibiting bronchospasm, peritoneal anaphylaxis, ear edema, and leukotriene production in animal models. Pharmacokinetic studies indicate a short half-life in monkeys (< 1 hour) and a longer half-life in humans (3 hours). However, Zileuton has been associated with potential liver toxicity, demonstrating elevated liver enzyme levels and moderate DILI severity in clinical datasets. Overall, Zileuton holds promise as an anti-inflammatory agent through its robust 5-LO inhibition, although its hepatotoxic potential warrants caution..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	Zileuton (A 64077) is a synthetic derivative of hydroxyurea with antiasthmatic properties. The leukotriene inhibitor zileuton blocks 5-lipoxygenase, which catalyzes the formation of leukotrienes from arachidonic acid; causes bronchodilation; decreases bronchial mucous secretion and edema; and may prevent or decrease the symptoms of asthma.
In vitro	Zileuton inhibited PGE2 production in lipopolysaccharide-stimulated human whole blood. In rat carrageenan gum-induced pleurisy, Zileuton decreased PGE2 and 6-ketoprostaglandin F1α pleural levels. In activated mouse peritoneal macrophages and macrophage J774, Zileuton significantly reduced PGE2 and 6-keto prostaglandin F1α levels. In macrophages, Zileuton inhibited PG biosynthesis by interfering with arachidonic acid release.
In vivo	Zileuton inhibited PGE2 production in lipopolysaccharide-stimulated human whole blood. In rat carrageenan gum-induced pleurisy, Zileuton decreased PGE2 and 6-ketoprostaglandin F1α pleural levels. In activated mouse peritoneal macrophages and macrophage J774, Zileuton significantly reduced PGE2 and 6-keto prostaglandin F1α levels. In macrophages, Zileuton inhibited PG biosynthesis by interfering with arachidonic acid release.
Synonyms	Abbott 64077, A 64077

Chemical Properties

Molecular Weight	236.29
Formula	C₁₁H₁₂N₂O₂S
Cas No.	111406-87-2
Smiles	C(N(C(N)=O)O)(C)C1=CC=2C(S1)=CC=CC2
Relative Density.	1.401 g/cm3

Storage & Solubility Information

Storage

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

Solubility Information

DMSO: 126 mg/mL (533.24 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 10 mg/mL (42.32 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	4.2321 mL	21.1604 mL	42.3209 mL	211.6044 mL
5 mM	0.8464 mL	4.2321 mL	8.4642 mL	42.3209 mL
10 mM	0.4232 mL	2.1160 mL	4.2321 mL	21.1604 mL
20 mM	0.2116 mL	1.0580 mL	2.1160 mL	10.5802 mL
50 mM	0.0846 mL	0.4232 mL	0.8464 mL	4.2321 mL
100 mM	0.0423 mL	0.2116 mL	0.4232 mL	2.1160 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 stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

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

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