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Zileuton

Cat. No. M2332
Zileuton Structure
Size Price Availability Quantity
10mg USD 50 In stock
50mg USD 130 In stock
100mg USD 205 In stock
500mg USD 480 In stock
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Quality Control
Biological Activity

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).

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 236.29
Formula C11H12N2O2S
CAS Number 111406-87-2
Purity >99%
Solubility DMSO 20 mg/mL
Storage at -20°C
References

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.

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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.

  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Zileuton supplier, Lipoxygenase, inhibitors

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