Zileuton is an orally active 5-LO (5-lipoxygenase) inhibitor that inhibits LTB4 synthesis (IC50 values are 0.56, 2.3 and 2.6 μM in dog, rat and human blood respectively). Zileuton inhibits antigen-induced contraction of tracheal strips in vitro (IC50 = 6 μM) and shows antiasthmatic activity in vivo. Zileuton also weakly inhibits CYP1A2 (Ki = 66 - 98 μM).
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.
Soluble in DMSO (47 mg/ml at 25° C), methanol, ethanol (47 mg/ml at 25° C), DMF (~30 mg/ml), and 1:1 DMSO:PBS(pH 7.2) (~0.5 mg/ml).
I Need to dilute Zileuton (CAS 111406-87-2) in Carboxymethylcellulose 0,5% to give to my rats by gavage in a dosage of 30 mg/kg. Do you have any suggestion how can I dilute it?
Thanks in advance.
Asked by: Marcell
Unfortunately we are not able to provide that information. Our compounds are not pharmaceutical grade and not manufactured under GMP guidelines. Please consult your principal investigator and your animal care and use committee (ACUC) regarding the use of our compounds.
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Kuvibidila et alKuvibidila et al. (PubMed ID 26412995) found that Zileuton likely reduced IL-2 secretion via inhibition of 5-lipoxygenase in patients with sickle cell disease. -SCBT Publication Review
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