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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).
| Molecular Weight | 236.29 |
| Formula | C11H12N2O2S |
| CAS Number | 111406-87-2 |
| Solubility (25°C) | DMSO ≥ 75 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Lipoxygenase Products |
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| Malotilate
Malotilate is a hepatoprotective agent used in the treatment of liver disease. |
| GSK2190915
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. |
| MK 886
Mk-886 (L 663536) is a potent, cellular permeable, orally active inhibitor of FLAP (IC50 at 30 nM) and leukotriene biosynthesis (IC50 at 3 nM and 1.1μM in whole white blood cells and human whole blood, respectively). Mk-886 is also a non-competitive PPARα antagonist that can induce apoptosis. |
| Picrinine
Picrinine is an Akuammiline alkaloid isolated from the leaves of Alstonia Scholaris. Picrinine shows anti-inflammatory activity by inhibiting 5-lipoxygenase. |
| 2-TEDC
2-TEDC is a 5-, 12-, 15-Lipoxygenase inhibitor. |
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