Catalog Number: 3308
Alternate Names: ICI D2138
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 (Ki = 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. All Tocris products are intended for laboratory research use only.
Background References
  1. 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
  2. The 5-lipoxygenase inhibitory activity of zileuton in in vitro and in vivo models of antigen-induced airway anaphylaxis.
    Malo et al.
    Pulm.Pharmacol., 1994;7:73
  3. 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

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