Biological Activity
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).
Compound Libraries
Zileuton is also offered as part of the Tocriscreen Plus and Tocriscreen Library of FDA-Approved Compounds. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 236.29 |
| Formula | C11H12N2O2S |
| Storage | Store at +4°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 111406-87-2 |
| PubChem ID | 60490 |
| InChI Key | MWLSOWXNZPKENC-UHFFFAOYSA-N |
| 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.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 23.63 | 100 |
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 |
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References
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
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