Filorexant

1088991-73-4

C24H25FN4O2

DMSO : 12.61 mg/mL (29.99 mM; Need ultrasonic)

GPCR/G Protein; Neuronal Signaling

Filorexant (MK-6096) is an orally bioavailable potent and selective reversible antagonist of OX1 and OX2 receptor(<3 nM in binding). IC50 & Target: Ki: < 3 nM(Orexin receptor)^[1]. In Vitro: 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. In Vivo: 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).