Art. -Nr.: HY-14164

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Zileuton

(Synonyms: A 64077; Abbott 64077)

24 Cited Publications

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Based on 24 publication(s) in Google Scholar

Zileuton is a potent and selective inhibitor of 5-lipoxygenase with antiasthmatic properties.

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Reinheit: 99.61%
CAS. Nr.: 111406-87-2
Formel: C₁₁H₁₂N₂O₂S
Molecular Weight:236.30

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months

Zileuton Chemical Structure

CAS. Nr.: 111406-87-2

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (24)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Zileuton is a potent and selective inhibitor of 5-lipoxygenase with antiasthmatic properties.

IC₅₀ & Target

5-LOX

Alle Lipoxygenase Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
BMMC	IC₅₀	>20 μM Compound: zileuton	Antiosteoclast activity in mouse BMM cells assessed as reduction of RANKL-induced osteoclasts differentiation by measuring TRAP positive multinucleated cells after 4 days by light microscopy Antiosteoclast activity in mouse BMM cells assessed as reduction of RANKL-induced osteoclasts differentiation by measuring TRAP positive multinucleated cells after 4 days by light microscopy	[PMID: 26432605]
HeLa	IC₅₀	0.04 μg/mL Compound: Zileuton	Antiallergic activity in Ca(2+)-stimulated differentiated human HeLa cells assessed as inhibition of cys-leukotriene release after 6 days by ELISA Antiallergic activity in Ca(2+)-stimulated differentiated human HeLa cells assessed as inhibition of cys-leukotriene release after 6 days by ELISA	[PMID: 19942440]
MC9	IC₅₀	0.55 μM Compound: zileuton	Inhibition of LTB4 production in mouse MC9 cells Inhibition of LTB4 production in mouse MC9 cells	[PMID: 18498150]
PMNL	IC₅₀	0.5 μM Compound: zileuton	Inhibition of 5-lipoxygenase in cell free S100 freshly isolated human PMNL cells assessed as inhibition of A23187-stimulated 5-LO product formation preincubated for 15 mins measured after 10 mins by HPLC analysis Inhibition of 5-lipoxygenase in cell free S100 freshly isolated human PMNL cells assessed as inhibition of A23187-stimulated 5-LO product formation preincubated for 15 mins measured after 10 mins by HPLC analysis	[PMID: 22551629]
RBL-1	IC₅₀	0.5 μM Compound: A-64077	The compound was tested for inhibitory activity against 5-Lipoxygenase in rat RBL-1 The compound was tested for inhibitory activity against 5-Lipoxygenase in rat RBL-1	[PMID: 1635053]
RBL-1	IC₅₀	100 nM Compound: 1, (A-64077)	Compound was tested for in vitro inhibition on broken RBL-1. Compound was tested for in vitro inhibition on broken RBL-1.	[PMID: 8709092]
RBL-1	IC₅₀	3.2 μM Compound: zileuton	Inhibitory concentration against 5-lipoxygenase in rat RBL-1 cells Inhibitory concentration against 5-lipoxygenase in rat RBL-1 cells	[PMID: 8831759]
RBL-1	IC₅₀	0.5 μM Compound: 1a	Inhibition of 5-lipoxygenase on rat basophil leukemia cell line lysate (RBL-1 2H3 subline) by measuring 5-HETE production Inhibition of 5-lipoxygenase on rat basophil leukemia cell line lysate (RBL-1 2H3 subline) by measuring 5-HETE production	[PMID: 9207936]
RBL-1	IC₅₀	0.14 μM Compound: A-64077 (Zileuton, 5)	Inhibition of 5-Lipoxygenase of rat basophilic leukemia cells Inhibition of 5-Lipoxygenase of rat basophilic leukemia cells	10.1016/S0960-894X(00)80622-8
RBL-2H3	IC₅₀	804 nM Compound: zileuton	Inhibition of 5-lipoxygenase mediated conversion of [14C]arachidonic acid to leukotrienes in RBL-2H3 cells Inhibition of 5-lipoxygenase mediated conversion of [14C]arachidonic acid to leukotrienes in RBL-2H3 cells	[PMID: 9599246]
RBL-2H3	IC₅₀	1.25 μM Compound: Zileuton	In vitro inhibition of 5-lipoxygenase in RBL-2H3 (Rat basophilic leukemia) cells. In vitro inhibition of 5-lipoxygenase in RBL-2H3 (Rat basophilic leukemia) cells.	10.1016/0960-894X(95)00088-B
Sf21	IC₅₀	564.4 μM Compound: Zileuton	Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake	[PMID: 21965623]
Sf21	IC₅₀	>1000 μM Compound: Zileuton	Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake	[PMID: 21965623]

In Vitro

In anti-CD3-treated cells, IL-2 decreases in zileuton-treated and untreated cells with increasing incubation time. Zileuton likely reduces IL-2 levels by inhibiting 5-lipoxygenase, hence leukotriene B4 production, an IL-2 inducer^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

In zileuton (5 mg/kg, p.o.) treated I/R rat, the effect of zileuton to decrease NF-κB expression does not change significantly in the presence of COX inhibitors, and the group reveals significantly lower level of NF-κB staining. Zileuton (5 mg/kg, p.o.) treatment given to I/R rats decreases apoptotic index significantly. Zileuton has no significant effect on increased serum TNF-α levels in I/R group^[1]. Zileuton (1,200 mg/kg) inhibits the polyp formation in APC^Δ468 colon and small intestine. Zileuton treatment inhibits the proliferation rates of non epithelial cells in polyps, and increases the apoptosis rates in polyps in rat. There is significant increase in the number of apoptotic cells in the Zileuton-treated cells both in small intestine and in the colon. The reduced proliferation rate may significantly contribute to the reduction of polyposis in both the small intestine and colon of Zileuton-fed APC^Δ468 mice^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 111406-87-2
Appearance Solid
Molecular Weight 236.30
Formel C₁₁H₁₂N₂O₂S
Color White to off-white
SMILES

CC(N(O)C(N)=O)C1=CC2=CC=CC=C2S1
Synonyms

A 64077; Abbott 64077
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Publications (24)

All Cell Proliferation/Viability AssayIFWB

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Journal Impact Factor

Sci Immunol

2026 May;11(119):eadz0348. PMID: 42066062
Nat Commun

A mouse protozoan boosts antigen-specific mucosal IgA responses in a specific lipid metabolism- and signaling-dependent manner. [Abstract]

2024 Sep 10;15(1):7914. PMID: 39256385
Redox Biol

Excessive linoleic acid induces muscle oxidative stress through 5-lipoxygenase-dependent peroxidation. [Abstract]

2024 May:71:103096. PMID: 38387137
MedComm (2020)

2026 Apr 9;7(4):e70722. PMID: 41969632
J Neuroinflammation

P2X7-CaMKII drives 5-LOX nuclear translocation to impair microglial function after subarachnoid hemorrhage. [Abstract]

2025 Aug 28;22(1):208. PMID: 40877894
Food Chem

2026 Jun 1:12:100426. PMID: 42291108
Cell Death Dis

A novel taxane SB-T-101141 triggers a noncanonical ferroptosis to overcome Paclitaxel resistance of breast cancer via iron homeostasis-related KHSRP. [Abstract]

2025 May 19;16(1):403. PMID: 40389408
J Cachexia Sarcopenia Muscle

A disease-associated missense mutation in CYP4F3 affects the metabolism of leukotriene B4 via disruption of electron transfer. [Abstract]

2022 Aug;13(4):2242-2253. PMID: 35686338
ACS Environ Au

Machine Learning-Assisted Recognition of Environmental Sulfur-Containing Chemicals in Nontargeted Mass Spectrometry Analysis of Inadequate Mass Resolution. [Abstract]

2025 Aug 5;5(6):573-582. PMID: 41277996
Emerg Microbes Infect

Gut dysbacteriosis attenuates resistance to Mycobacterium bovis infection by decreasing cyclooxygenase 2 to inhibit endoplasmic reticulum stress. [Abstract]

2022 Dec;11(1):1806-1818. PMID: 35766265
Anal Chem

Exposome-Scale Investigation of Cl-/Br-Containing Chemicals Using High-Resolution Mass Spectrometry, Multistage Machine Learning, and Cloud Computing. [Abstract]

2025 Jun 3;97(21):11099-11109. PMID: 40401576
J Ethnopharmacol

Involvement of p38 MAPK/cPLA2 and arachidonic acid metabolic pathway in Shengmai injection-induced pseudo-allergic reactions. [Abstract]

2023 Jun 12:309:116357. PMID: 36906156
Int J Mol Sci

Zileuton, a 5-Lipoxygenase Inhibitor, Attenuates Haemolysate-Induced BV-2 Cell Activation by Suppressing the MyD88/NF-κB Pathway. [Abstract]

2022 Apr 28;23(9):4910. PMID: 35563304
Front Cell Infect Microbiol

Dysregulation of Cytosolic c-di-GMP in Edwardsiella piscicida Promotes Cellular Non-Canonical Ferroptosis. [Abstract]

2022 Feb 4;12:825824. PMID: 35186798
J Cell Mol Med

Downregulation of Alox5 Inhibits Ferroptosis to Improve Doxorubicin-Induced Cardiotoxicity via the P53/SLC7A11 Pathway. [Abstract]

2025 Jun;29(11):e70641. PMID: 40485049
Proteomics

Integrative Analysis of Proteome and Ubiquitylome Reveals Unique Features of Lysosomal and Endocytic Pathways in Gefitinib-Resistant Non-Small Cell Lung Cancer Cells. [Abstract]

2018 Aug;18(15):e1700388. PMID: 29901268

Zileuton purchased from MedChemExpress. Usage Cited in: Proteomics. 2018 Aug;18(15):e1700388. [Abstract]

Comparison of Gefitinib resistant colony formation between PC9/GR cells treated with the control (DMSO) or 200uM Zileuton.
Toxicol Appl Pharmacol

2026 Jun:511:117821. PMID: 41967610
Head Neck

iPLA2β regulates the dual effects of arachidonic acid in thyroid cancer. [Abstract]

2025 Feb;47(2):504-516. PMID: 39290130
Biochem Biophys Res Commun

Effects of intracellular iron overload on cell death and identification of potent cell death inhibitors. [Abstract]

2018 Sep 3;503(1):297-303. PMID: 29890135
Northwestern University

2026.
University of Padua

2024.
bioRxiv

Rebalancing Viral and Immune Damage versus Tissue Repair Prevents Death from Lethal Influenza Infection. [Abstract]

2024 Jul 7:2024.07.04.601620. PMID: 39372755
Oxid Med Cell Longev

Cepharanthine Attenuates Early Brain Injury after Subarachnoid Hemorrhage in Mice via Inhibiting 15-Lipoxygenase-1-Mediated Microglia and Endothelial Cell Ferroptosis. [Abstract]

2022 Feb 9;2022:4295208. PMID: 35186185
Oxid Med Cell Longev

The 5-Lipoxygenase Inhibitor Zileuton Protects Pressure Overload-Induced Cardiac Remodeling via Activating PPAR α. [Abstract]

2019 Nov 3;2019:7536803. PMID: 31781348

Zileuton purchased from MedChemExpress. Usage Cited in: Oxid Med Cell Longev. 2019 Nov 3;2019:7536803. [Abstract]

Zileuton inhibits oxidative stress in cardiomyocytes. H9c2 cells are treated with PE (50 μM) and zileuton (100 μM) for 24 h. ROS levels in H9c2 cells (n = 6).

Zileuton purchased from MedChemExpress. Usage Cited in: Oxid Med Cell Longev. 2019 Nov 3;2019:7536803. [Abstract]

Zileuton inhibits oxidative stress in cardiomyocytes. H9c2 cells are treated with PE (50 μM) and zileuton (100 μM) for 24 h. ROS levels in H9c2 cells (n = 6).

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (423.19 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

4.2319 mL

21.1595 mL

42.3191 mL

5 mM

0.8464 mL

4.2319 mL

8.4638 mL

10 mM

0.4232 mL

2.1160 mL

4.2319 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 10 mg/mL (42.32 mM); Clear solution

This protocol yields a clear solution of ≥ 10 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (100.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 10 mg/mL (42.32 mM); Clear solution

This protocol yields a clear solution of ≥ 10 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (100.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 10 mg/mL (42.32 mM); Clear solution

This protocol yields a clear solution of ≥ 10 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (100.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 50% PEG300 50% Saline

Solubility: 5 mg/mL (21.16 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protokoll

Animal Administration^[1]

Rats: Rats are randomized into 6 groups (n=12 per group): sham I/R group, I/R group, zileuton+I/R group, zileuton+indomethacin+I/R group, zileuton+ketorolac+I/R group, and zileuton+nimesulide+I/R group. 5-LOX inhibitor zileuton (5 mg/kg, orally twice daily) is given alone or with non-selective COX inhibitor indomethacin (5 mg/kg, intraperitoneally), selective COX-1 inhibitor ketorolac (10 mg/kg, orally) or selective COX-2 inhibitor nimesulide (10 mg/kg, subcutaneously). COX inhibitors are given 15 minutes before zileuton administration. All drugs are given for 3 days prior to I/R or sham I/R procedure. Dose of zileuton (5 mg/kg, twice daily) is used in this study. Rats in sham I/R group receive the vehicle of zileuton orally. Zileuton is dissolved in dimethyl sulfoxide (DMSO) and further dilutions are made using saline to achieve a final DMSO concentration of 1%.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (280 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Abueid L, et al. Inhibition of 5-lipoxygenase by zileuton in a rat model of myocardial infarction. Anatol J Cardiol. 2016 Nov 10 [Content Brief]

[2]. Kuvibidila S, et al. Hydroxyurea and Zileuton Differentially Modulate Cell Proliferation and Interleukin-2 Secretion by Murine Spleen Cells: Possible Implication on the Immune Function and Risk of Pain Crisis in Patients with Sickle Cell Disease. Ochsner [Content Brief]

[3]. Gounaris E, et al. Zileuton, 5-lipoxygenase inhibitor, acts as a chemopreventive agent in intestinal polyposis, by modulating polyp and systemic inflammation. PLoS One. 2015 Mar 6;10(3):e0121402 [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	4.2319 mL	21.1595 mL	42.3191 mL	105.7977 mL
	5 mM	0.8464 mL	4.2319 mL	8.4638 mL	21.1595 mL
	10 mM	0.4232 mL	2.1160 mL	4.2319 mL	10.5798 mL
	15 mM	0.2821 mL	1.4106 mL	2.8213 mL	7.0532 mL
	20 mM	0.2116 mL	1.0580 mL	2.1160 mL	5.2899 mL
	25 mM	0.1693 mL	0.8464 mL	1.6928 mL	4.2319 mL
	30 mM	0.1411 mL	0.7053 mL	1.4106 mL	3.5266 mL
	40 mM	0.1058 mL	0.5290 mL	1.0580 mL	2.6449 mL
	50 mM	0.0846 mL	0.4232 mL	0.8464 mL	2.1160 mL
	60 mM	0.0705 mL	0.3527 mL	0.7053 mL	1.7633 mL
	80 mM	0.0529 mL	0.2645 mL	0.5290 mL	1.3225 mL
	100 mM	0.0423 mL	0.2116 mL	0.4232 mL	1.0580 mL

Keywords

Zileuton

24 Cited Publications

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Zileuton

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Publications Citing Use of MedChemExpress (MCE) Zileuton

Alle Lipoxygenase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (24)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Zileuton Related Classifications

HY-14164 Related Classifications