Filorexant 是一种口服有效且选择性可逆的 OX1 和 OX2 受体拮抗剂，Ki值小于3nM。

Filorexant occupies 90% of human OX(2)Rs expressed in transgenic rats at a plasma concentration of 142 nM. Filorexant demonstrated effective binding and antagonism of both human OX(1)R and OX(2)R (<3 nM in binding, 11 nM in FLIPR), in radioligand binding and functional cell-based assays. It has no significant off-target activities against a panel of >170 receptors and enzymes [1].

Filorexant is an orally bioavailable effective and selective reversible antagonist of OX1 and OX2 receptor with (Ki<3 nM).

Filorexant occupies 90% of human OX(2)Rs expressed in transgenic rats at a plasma concentration of 142 nM. Filorexant demonstrated effective binding and antagonism of both human OX(1)R and OX(2)R (<3 nm in binding, 11 flipr), radioligand binding and functional cell-based assays. it has no significant off-target activities against a panel of>170 receptors and enzymes [1].

Filorexant dose-dependently decreased locomotor activity and obviously enhanced sleep in rats (3-30 mg/kg) and dogs (0.25 and 0.5 mg/kg)[1].

1088991-73-4

C24H25FN4O2

420.48

MK-6096

DMSO:100 mg/mL (237.82 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years