Filorexant

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Filorexant 是一种口服生物可利用的有效且选择性可逆的 OX1 和 OX2 受体拮抗剂（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

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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

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(-20℃)

With Ice Pack

≥ 2 years