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.
| Molecular Weight | 472.08 |
| Formula | C27H34ClNO2S |
| CAS Number | 118414-82-7 |
| Solubility (25°C) | DMSO 90 mg/mL Ethanol 5 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 |
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| 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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