Zileuton (trade name ZYFLO) is an orally active inhibitor of 5-lipoxygenase, and thus inhibits leukotrienes (LTB4, LTC4, LTD4, and LTE4) formation. Zileuton inhibits 5-LO from rat basophilic leukemia-1 (RBL-1) cells with an IC50 value of 0.5 µM. Zileuton inhibits antigen-induced contraction of tracheal strips in vitro (IC50 = 6 μM) and exhibits antiasthmatic activity in vivo. Zileuton also weakly inhibits CYP1A2 (Ki = 66 - 98 μM). Zileuton is used for the maintenance treatment of asthma. Research on mice suggests that Zileuton used alone or in combination with imatinib may inhibit chronic myeloid leukemia (CML).
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
|Solubility||DMSO 25 mg/mL|
Mechanism-based inhibition of human liver microsomal cytochrome P450 1A2 by zileuton, a 5-lipoxygenase inhibitor.
Lu P, et al. Drug Metab Dispos. 2003 Nov;31(11):1352-60. PMID: 14570767.
The 5-lipoxygenase inhibitory activity of zileuton in in vitro and in vivo models of antigen-induced airway anaphylaxis.
Malo PE, et al. Pulm Pharmacol. 1994 Apr;7(2):73-9. PMID: 8081074.
|Related Lipoxygenase Products|
FPL 62064 is a potent dual inhibitor of 5-lipoxygenase (5-LOX) and prostaglandin synthetase (cyclooxygenase, COX) with IC50 of 3.5 μM and 3.1 μM for RBL-1 cytosolic 5-lipoxygenase and seminal vesicle prostaglandin synthetase, respectively.
AKBA is an active triterpenoid compound from the extract of Boswellia serrata and Boswellia carteri Birdw, exerts anti-inflammatory therapeutic effects and noncompetitively inhibits 5-lipoxygenase, topoisomerase, and leukocyte elastase.
BHQ is a inhibitor of SERCA ATPase.
MK 886 is a potent 5-lipoxygenase activating protein inhibitor (FLAP) (IC50 = 44 nM).
GSK2190915 (AM803), a potent FLAP inhibitor, prevents the synthesis of leukotrienes and 5-oxo-ETE, with IC50 of 76 nM for inhibition of LTB4 in human blood, provides treatment for asthma.
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