Filorexant

Research use only, not for human use.

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

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

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).

MK-6096

Others

Other Targets

——

——

——

1088991-73-4

420.488

C24H25FN4O2

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (237.82 mM)

C[C@@H]1CC[C@@H](COc2ccc(F)cn2)CN1C(=O)c1cc(C)ccc1-c1ncccn1

——

(-20℃)

With Ice Pack

≥ 2 years