Zileuton
Chemical Name: N-(1-Benzo[b]thien-2-ylethyl)-N-hydroxyurea
Purity: ≥99%
Biological Activity
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.Technical Data
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.
Background References
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Pre-clinical pharmacology of ICI D2138, a potent orally-active non-redox inhibitor of 5-lipoxygenase.
McMillan et al.
Br.J.Pharmacol., 1992;107:1042 -
Mechanism-based inhibition of human liver microsomal cytochrome P450 1A2 by zileuton, a 5-lipoxygenase inhibitor.
Lu et al.
Drug Metab.Dispos., 2003;31:1352 -
Ferroptosis: process and function.
Xie et al.
Cell.Death.Differ, 2016;23:369 -
The 5-lipoxygenase inhibitory activity of zil. in in vitro and in vivo models of antigen-induced airway anaphylaxis.
Malo et al.
Pulm.Pharmacol., 1994;7:73
Product Datasheets
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Citations for Zileuton
The citations listed below are publications that use Tocris products. Selected citations for Zileuton include:
7 Citations: Showing 1 - 7
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The Investigation of Lipoxygenases as Therapeutic Targets in Malignant Pleural Mesothelioma.
Authors: Oguh-Olayinka Et al.
Pathol Oncol Res 2019;
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Activation of Glutathione Peroxidase 4 as a Novel Anti-inflammatory Strategy.
Authors: Li Et al.
Front Pharmacol 2018;9:1120
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The Kaposi's sarcoma-associated herpesvirus (KSHV)-induced 5-lipoxygenase-leukotriene B4 cascade plays key roles in KSHV latency, monocyte recruitment, and lipogenesis.
Authors: Sharma-Walia Et al.
J Virol 2014;88:2131
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The role of cyclooxygenase-derived oxidative stress in surgically induced lymphedema in a mouse tail model.
Authors: Chang Et al.
Pharm Biol 2013;51:573
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Adipocytes secrete leukotrienes: contribution to obesity-associated inflammation and Ins resistance in mice.
Authors: Mothe-Satney Et al.
Diabetes 2012;61:2311
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Spinal 12-lipoxygenase-derived hepoxilin A3 contributes to inflammatory hyperalgesia via activation of TRPV1 and TRPA1 receptors.
Authors: Gregus Et al.
Proc Natl Acad Sci U S A 2012;109:6721
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Natural forms of vitamin E and 13'-carboxychromanol, a long-chain vitamin E metabolite, inhibit leukotriene generation from stimulated neutrophils by blocking calcium influx and suppressing 5-lipoxygenase activity, respectively.
Authors: Jiang Et al.
J Immunol 2011;186:1173
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