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Zileuton

Cat No. 3308

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Chemical Name: N-(1-Benzo[b]thien-2-ylethyl)-N-hydroxyurea

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 (K_i = 66 - 98 μM).

Technical Data

M.Wt:

236.29

Formula:

C₁₁H₁₂N₂O₂S

Solubility:

Soluble to 100 mM in DMSO

Purity:

>99 %

Storage:

Store at +4°C

CAS No:

[111406-87-2]

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

Resources

Certificate of Analysis / MSDS

Certificate of Analysis: View current batch

Material Safety Data Sheet: View current batch

References

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. 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. 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.

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