产品信息
抗原名称
OX2 receptor,OX1 receptor
商品描述
Almorexant(ACT078573) is a potent and competitive dual orexin 1 receptor (OX1)/orexin 2 receptor (OX2) antagonist with Ki values of 1.3 and 0.17 nM for OX1 and OX2, respectively.
分子量
549.02
纯度
>98%
可溶性
DMSO 72 mg/mL (131.14 mM)
Ethanol 51 mg/mL (92.89 mM)
Ethanol 51 mg/mL (92.89 mM)
外观
Powder
In vitro(体外研究)
Almorexant inhibits the increase in intracellular Ca2+ induced by 10 nM human orexin-A in Chinese hamster ovary cells with IC50 of 16 nM (rat) and 13 nM (human) for the OX1 receptor and 15 nM (rat) and 8 nM (human) for the OX2 receptor.
In vivo(体内研究)
Almorexant (300 mg/kg p.o.) decreases alertness, and increases electrophysiological indices of both non-REM and REM sleep in male Wistar rats. In dogs, Almorexant (100 mg/kg p.o.) causes somnolence and increases surrogate markers of REM sleep. Almorexant induces a robust antidepressant-like effect and the restoration of stress-related HPA axis defect independently from a neurogenic action. In addition, Almorexant also reduces ethanol self-administration in high-drinking rodent models.
背景
别名
ACT-078573; ACT 078573; ACT078573;ACT-078573 hydrochloride; ACT 078573 hydrochloride; ACT078573 hydrochloride
分子式
C29H32ClF3N2O3
CAS号
913358-93-7
制备和贮存
保存方式
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
参考图片
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