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Description: 5-LOX inhibitor; orally bioavailable
Alternative Names: ICI D2138
Chemical Name: N-(1-Benzo[b]thien-2-ylethyl)-N-hydroxyurea
Purity: ≥99% (HPLC)
Citations (7)
Literature (2)

Biological Activity for Zileuton

Zileuton is an orally active 5-lipoxygenase (5-LOX) inhibitor that inhibits LTB4 synthesis (IC50 values are 0.56, 2.3 and 2.6 μM in dog, rat and human blood respectively). Inhibits antigen-induced contraction of tracheal strips in vitro (IC50 = 6 μM) and exhibits antiasthmatic activity in vivo. Also weakly inhibits CYP1A2 (Ki = 66 - 98 μM). Ferroptosis inhibitor.

Compound Libraries for Zileuton

Zileuton is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen FDA-Approved Drugs. Find out more about compound libraries available from Tocris.

Technical Data for Zileuton

M. Wt 236.29
Formula C11H12N2O2S
Storage Store at +4°C
Purity ≥99% (HPLC)
CAS Number 111406-87-2
PubChem ID 60490
Smiles CC(N(O)C(N)=O)C2=CC1=CC=CC=C1S2

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for Zileuton

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 23.63 100

Preparing Stock Solutions for Zileuton

The following data is based on the product molecular weight 236.29. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 4.23 mL 21.16 mL 42.32 mL
5 mM 0.85 mL 4.23 mL 8.46 mL
10 mM 0.42 mL 2.12 mL 4.23 mL
50 mM 0.08 mL 0.42 mL 0.85 mL

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References for Zileuton

References are publications that support the biological activity of the product.

McMillan et al (1992) Pre-clinical pharmacology of ICI D2138, a potent orally-active non-redox inhibitor of 5-lipoxygenase. Br.J.Pharmacol. 107 1042 PMID: 1334748

Malo et al (1994) The 5-lipoxygenase inhibitory activity of zil. in in vitro and in vivo models of antigen-induced airway anaphylaxis. Pulm.Pharmacol. 7 73 PMID: 8081074

Lu et al (2003) Mechanism-based inhibition of human liver microsomal cytochrome P450 1A2 by zileuton, a 5-lipoxygenase inhibitor. Drug Metab.Dispos. 31 1352 PMID: 14570767

Xie et al (2016) Ferroptosis: process and function. Cell Death Differ. 23 269 PMID: 26794443

If you know of a relevant reference for Zileuton, please let us know.

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Keywords: Zileuton, Zileuton supplier, Orally, active, 5-LOX, inhibitors, inhibits, Lipoxygenase, Oxygenases, Oxidases, ICID2138, ferroptosis, ICI, D2138, Ferroptosis, 3308, Tocris Bioscience

⚠ WARNING: This product can expose you to chemicals including Zileuton, which is known to the State of California to cause reproductive toxicity with developmental effects. For more information, go to www.P65Warnings.ca.gov

7 Citations for Zileuton

Citations are publications that use Tocris products. Selected citations for Zileuton include:

Gregus et al (2012) Spinal 12-lipoxygenase-derived hepoxilin A3 contributes to inflammatory hyperalgesia via activation of TRPV1 and TRPA1 receptors. Proc Natl Acad Sci U S A 109 6721 PMID: 22493235

Mothe-Satney et al (2012) Adipocytes secrete leukotrienes: contribution to obesity-associated inflammation and Ins resistance in mice. Diabetes 61 2311 PMID: 22688342

Chang et al (2013) The role of cyclooxygenase-derived oxidative stress in surgically induced lymphedema in a mouse tail model. Pharm Biol 51 573 PMID: 23373707

Li et al (2018) Activation of Glutathione Peroxidase 4 as a Novel Anti-inflammatory Strategy. Front Pharmacol 9 1120 PMID: 30337875

Do you know of a great paper that uses Zileuton from Tocris? Please let us know.

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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

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