For research use only. Not for therapeutic Use.
Filorexant (MK-6096) is an orally bioavailable potent and selective reversible antagonist of OX1 and OX2 receptor(<3 nM in binding).
In radioligand binding and functional cell based assays Filorexant (MK-6096) demonstrated potent binding and antagonism of both human OX(1)R and OX(2)R (<3 nM in binding, 11 nM in FLIPR), with no significant off-target activities against a panel of >170 receptors and enzymes. Filorexant (MK-6096) occupies 90% of human OX(2)Rs expressed in transgenic rats at a plasma concentration of 142 nM.
Filorexant (MK-6096) dose-dependently reduced locomotor activity and significantly increased sleep in rats (3-30 mg/kg) and dogs (0.25 and 0.5 mg/kg).
| Catalog Number | I000376 |
| CAS Number | 1088991-73-4 |
| Synonyms | [(2R,5R)-5-[(5-fluoropyridin-2-yl)oxymethyl]-2-methylpiperidin-1-yl]-(5-methyl-2-pyrimidin-2-ylphenyl)methanone |
| Molecular Formula | C24H25FN4O2 |
| Purity | ≥95% |
| InChI | InChI=1S/C24H25FN4O2/c1-16-4-8-20(23-26-10-3-11-27-23)21(12-16)24(30)29-14-18(6-5-17(29)2)15-31-22-9-7-19(25)13-28-22/h3-4,7-13,17-18H,5-6,14-15H2,1-2H3/t17-,18-/m1/s1 |
| InChIKey | NPFDWHQSDBWQLH-QZTJIDSGSA-N |
| SMILES | CC1CCC(CN1C(=O)C2=C(C=CC(=C2)C)C3=NC=CC=N3)COC4=NC=C(C=C4)F |
| Reference | [1]. Winrow CJ, et al. Pharmacological characterization of MK-6096 – a dual orexin receptor antagonist for insomnia. Neuropharmacology. 2012 Feb;62(2):978-87. [2]. Coleman PJ, et al. Discovery of [(2R,5R)-5-{[(5-fluoropyridin-2-yl)oxy]methyl}-2-methylpiperidin-1-yl][5-methyl-2-(pyrimidin-2-yl)phenyl]methanone (MK-6096): a dual orexin receptor antagonist with potent sleep-promoting properties. ChemMedChem. 2012 Mar 5 |
