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).
|Storage||Store at +4°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 236.29. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
|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|
References are publications that support the products' biological activity.
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 zileuton 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
If you know of a relevant reference for Zileuton, please let us know.
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Keywords: Zileuton, supplier, Orally, active, 5-LOX, inhibitors, inhibits, Lipoxygenase, Oxygenases, Oxidases, ICID2138, 5-LOX, ferroptosis, inhibitors, inhibits, ICI, D2138, Lipoxygenase, Ferroptosis, Lipoxygenase, Tocris Bioscience
4 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 insulin resistance in mice. Diabetes 61 2311 PMID: 22688342
Jiang et al (2011) 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. J Immunol 186 1173 PMID: 21169551
Sharma-Walia et al (2014) The Kaposi's sarcoma-associated herpesvirus (KSHV)-induced 5-lipoxygenase-leukotriene B4 cascade plays key roles in KSHV latency, monocyte recruitment, and lipogenesis. J Virol 88 2131 PMID: 24335295
Do you know of a great paper that uses Zileuton from Tocris? If so please let us know.
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