Quiflapon (MK-591) is a selective and specific 5-lipoxygenase-activating protein (FLAP) inhibitor with an IC50 of 1.6 nM in a FLAP binding assay. Quiflapon is also a potent and orally active Leukotriene biosynthesis (LT) inhibitor, shows IC50 values of 3.1 and 6.1 nM in intact human and elicited rat PMNLs, respectively. Quiflapon induces cell apoptosis.
| Molecular Weight | 587.17 |
| Formula | C34H35ClN2O3S |
| CAS Number | 136668-42-3 |
| Form | Solid |
| Solubility (25°C) | DMSO ≥ 50 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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