| Description | Filorexant (MK-6096) is an orally bioavailable effective and selective reversible antagonist of OX1 and OX2 receptor with (Ki <3 nM). |
| In vitro | Filorexant在浆液浓度为142 nM时，占据了转基因大鼠表达的人类OX(2)R的90%。Filorexant在放射配体结合和功能性细胞基础试验中显示出对人类OX(1)R和OX(2)R的有效结合和拮抗作用（结合中<3 nM，FLIPR中11 nM）。Filorexant对于超过170种受体和酶的面板没有显著的非目标活性[1]。 |
| In vivo | Filorexant 在大鼠（3-30 mg/kg）和狗（0.25 和 0.5 mg/kg）中剂量依赖性地降低了运动活性，并显著增强了睡眠[1]。 |
| Target activity | OX receptor:< 3 nM(Ki) |
| Synonyms | MK-6096 |
| molecular weight | 420.48 |
| Molecular formula | C24H25FN4O2 |
| CAS | 1088991-73-4 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 100 mg/mL (237.82 mM), Sonication is recommended. |
| References | 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;7(3):415-24, 337. |