Zileuton Inhibitor CAS No. 111406-87-2

Cat. No.	Name	Size	Price	Add Cart
KI0731	Zileuton	20 mg	$154

Chemical Characteristic

Product Name	Zileuton
Synonyms	ZYFLO
CAS No.	111406-87-2
Molecular Weight	236.29
Formula	C₁₁H₁₂N₂O₂S
Chemical Name	1-(1-(benzo[b]thiophen-2-yl)ethyl)-1-hydroxyurea
Smiles	N(C(=O)N)(O)C(C)c1cc2c(s1)cccc2
Chemical Structure

Biological activities

Zileuton is an orally active 5-lipoxygenase inhibitor. Zileuton represents the first of a new class of medications to be used in the treatment of asthma.^[1] Zileuton also has been shown to be a weak inhibitor of human liver microsomal CYP3A4, CYP2C9, and CYP2D6 activity in vitro. Zileuton inhibits (??0%) theophylline metabolism at a final concentration of 100 µM. ^[2] Zileuton inhibits bron-choconstriction induced by cold, dry air inhalation and inhibits LT synthesis induced by nasal antigen challenge. ^[3] Zileuton inhibits 5-hydroxyeicosatetragnoic acid synthesis by rat basophilic leukemia cell 20,000 g supernatant and rat polymorphonuclear leukocytes (PMNL) with IC50 of 0.5 and 0.3 µM, respectively. Zileuton also inhibits leukotriene (LT)B_{4 biosynthesis by rat PMNL, human PMNL and human whole blood with IC50 of 0.4, 0.4 and 0.9 µM, respectively. At p.o. doses to from 0.5 to 5 mg/kg in the dog, zileuton produces a rapid and sustained inhibition of ex vivo blood LTB_{4 biosynthesis which correlated with the pharmacokinetic behavior of the zileuton. In a similar ex vivo study in the rat, zileuton displays an ED_{50 of 2 mg/kg. Zileuton is highly effective in preventing 6-sulfidopeptide LT formation in the rat peritoneal cavity triggered by an antigen-antibody reaction with an ED_{50 of 3 mg/kg. In experimental models of inflammation, zileuton significantly reduced arachidonic-acid induced mouse ear edema with an ED_{50 of 31 mg/kg. Zileuton also attenuates inflammatory cell accumulation in the rat pleural Arthus reaction. ^[4] In vivo guinea-pigs models of antigen-induced airway anaphylaxis, orally administered zileuton potently inhibits antigen-induced bronchoconstriction with an ED_{50 of 12 mg/kg. ^[5] In arachidonic acid-induced mouse ear oedema in vivo, zileuton produces dose-dependent inhibition of oedema with an ID50 value of 18 mg/kg p.o. In allergic bronchospasm in the guinea-pig in vivo, intravenous administration of zileuton also causes a dose-dependent inhibition of the antigen-induced increase in ventilatory pressure with an ID50 value of approximately 1.0 mg/kg.^[1] Zileuton treatment (10 mg/kg) also blocks antigen-induced late airway responses, inflammation and airway hyperresponsiveness in allergic sheep. ^[6]}}}}}}

Protocols

Zileuton is dissolved in DMSO. ^[4]

References

[1] Wenzel SE, et al. Zileuton: the first 5-lipoxygenase inhibitor for the treatment of asthma. Ann Pharmacother. 1996, 30(7-8): 858-864. [2] Lu P, et al. Mechanism-based inhibition of human liver microsomal cytochrome P450 1A2 by zileuton, a 5-lipoxygenase inhibitor. Drug Metab Dispos. 2003, 31(11): 1352-1360. [3] Kane GC, et al. A controlled trial of the effect of the 5-lipoxygenase inhibitor, zileuton, on lung inflammation produced by segmental antigen challenge in human beings. J Allergy Clin Immunol. 1996, 97(2): 646-654. [4] Carter GW, et al. 5-lipoxygenase inhibitory activity of zileuton. J Pharmacol Exp Ther. 1991, 256(3): 929-937. [5] Malo PE, et al. The 5-lipoxygenase inhibitory activity of zileuton in in vitro and in vivo models of antigen-induced airway anaphylaxis. Pulm Pharmacol. 1994, 7(2): 73-79. [6] Abraham WM, et al. The 5-lipoxygenase inhibitor zileuton blocks antigen-induced late airway responses, inflammation and airway hyperresponsiveness in allergic sheep. Eur J Pharmacol. 1992, 217(2-3): 119-126.

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