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Zileuton

Basic information Description References Safety Related Supplier
Zileuton Basic information
Zileuton Chemical Properties
  • Melting point:157-158°C
  • Boiling point:449.4±47.0 °C(Predicted)
  • Density 1.401±0.06 g/cm3(Predicted)
  • storage temp. Store at +4°C
  • solubility DMSO: ≥20mg/mL at ~60°C (warm up to 60 C for 5min)
  • pkapKa 10.3(H2O t undefined I undefined) (Uncertain)
  • form powder
  • color white to off-white
  • CAS DataBase Reference111406-87-2(CAS DataBase Reference)
Safety Information
  • Hazard Codes Xn
  • Risk Statements 22-36
  • Safety Statements 26
  • WGK Germany 1
  • HS Code 2934990002
MSDS
Zileuton Usage And Synthesis
  • DescriptionZileuton, a benzothiophene N-hydroxyurea, is the only approved inhibitor of 5-lipoxygenase. It is believed to intervene with allergic and inflammatory diseases by suppression of leukotriene (LT) biosynthesis. The compound belongs to the class of iron ligand-type inhibitors of 5-lipoxygenase that not only chelates the active site iron of the enzyme but also possesses weak-reducing properties.
    Zileuton is used as a type of drug for the prophylaxis and chronic treatment of asthma.
  • References[1] A Rossi, C Pergola, A Koeberle, M Hoffmann, F Dehm, P Bramanti, S Cuzzocrea, O Werz and L Sautebin, The 5-lipoxygenase inhibitor, zileuton, suppresses prostaglandin biosynthesis by inhibition of arachidonic acid release in macrophages, British Journal of Pharmacology, 2010, col. 161, 555-570
    [2] SE Wenzel and AK Kamada, Zileuton: the first 5-lipoxygenase inhibitor for the treatment of asthma, Ann Pharmacother., 1996, vol. 30, 858-864
  • DescriptionZyflo was launched in the US for chronic asthma. It can be prepared in three steps from 2-acetylbenzo[b]thiophene. Zyflo is a reversible direct inhibitor of 5- lipoxgenase that is orally-active. It was able to effect a 70-100 YO reduction in LTB4, LTE4, LTD4 and LTC4. Zyflo has no effect on myeloperoxidase activity, neutrophil degranulation, mast cell histamine release or phospholipase A2 activities. It did not inhibit cyclooxygenase as witnessed by the formation of TXB2. It significantly attentuated asthmatic response to cold dry air, inhibited exercise-induce bronchoconstriction, and attenuated induced bronchospasms. Zyflo has antiinflammatory effects as witnessed by a decrease in edema, mucus production and cellular infiltration. It had a bronchodilatory effect within 2 h and increased spirometry results by 18%.
  • Chemical PropertiesCrystalline Solid
  • OriginatorAbbott (US)
  • UsesAn inhibitor of 5-lipoxygenase, the initial enzyme in the biosynthesis of leukotrienes from Arachidonic Acid. Used as an antiasthmatic
  • Usesgastric acid secretion inhibitor
  • DefinitionChEBI: A member of the class of 1-benzothiophenes that is 1-benzothiophene in which the hydrogen at position 2 is replaced by a 1-[carbamoyl(hydroxy)amino]ethyl group. A selective 5-lipoxygenase inhibitor, it inhibits the formation of leukotrienes LTB4, LTC4, LDT , and LTE4. It is used for the management of chronic asthma.
  • brand nameZyflo (Sensus).
  • Biological ActivityOrally active 5-lipoxygenase (5-LOX) inhibitor that inhibits LTB 4 synthesis (IC 50 values are 0.56, 2.3 and 2.6 μ M in dog, rat and human blood respectively). Inhibits antigen-induced contraction of tracheal strips in vitro (IC 50 = 6 μ M) and exhibits antiasthmatic activity in vivo . Also weakly inhibits CYP1A2 (K i = 66 - 98 μ M).
Zileuton Preparation Products And Raw materials
Zileuton(111406-87-2)Related Product Information
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