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 |
| 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 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.
| Related Lipoxygenase Products |
|---|
| ALOX15-IN-2
ALOX15-IN-2 is a potent inhibitor of rabbit and human ALOX15 linoleate oxygenase activity, with IC50s of 1.55 and 2.79 μM for linoleic acid (LA) and arachidonic acid (AA), the immediate homologs of ALOX15, respectively. |
| Atractylochromene
Atractylochromene is a potent dual inhibitor of 5-LOX/COX-1 with IC50s of 0.6 and 3.3 μM, respectively. |
| 5-LOX-IN-5
5-LOX-IN-5 is a 5-LOX inhibitor (IC50: 56 nM). |
| EP6
EP6 is a potent 5-Lipoxygenase (5-LO) inhibitor. |
| Patulitrin
Patulitrin has scavenging effect in the DPPH radical. |
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