5-O-Demethylnobiletin (5-Demethylnobiletin), a polymethoxyflavone isolated from Sideritis tragoriganum, is a direct inhibition of 5-LOX (IC50=0.1 μM), without affecting the expression of COX-2. 5-O-Demethylnobiletin (5-Demethylnobiletin) has anti-inflammatory activity, inhibits leukotriene B (4)(LTB4) formation in rat neutrophils and elastase release in human neutrophils with an IC50 of 0.35 μM.
| Molecular Weight | 388.37 |
| CAS Number | 2174-59-6 |
| Solubility (25°C) | DMSO 25 mg/mL |
| Storage | 2-8°C, protect from light |
| 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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