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Almorexant hydrochloride
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Almorexant hydrochloride图片
CAS NO:913358-93-7
包装:10 mg
市场价:1949元

产品名称
Almorexant HCl
ACT-078573 hydrochloride
产品介绍
Almorexant hydrochloride 是一种有效的竞争性食欲素 1 受体 (OX1)/食欲素 2 受体 (OX2) 双重拮抗剂,OX1 和 OX2 的 Ki 值分别为 1.3 和 0.17 nM。

产品描述

Almorexant HCl (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.

体外活性

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. [1]

体内活性

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. [1] Almorexant induces a robust antidepressant-like effect and the restoration of stress-related HPA axis defect independently from a neurogenic action. [2] In addition, Almorexant also reduces ethanol self-administration in high-drinking rodent models. [3]

Cas No.

913358-93-7

分子式

C29H32ClF3N2O3

分子量

549.03

别名

Almorexant HCl;ACT-078573 hydrochloride

储存和溶解度

H2O:<1 mgml
Ethanol:48 mg/mL (87.4 mM)
DMSO:67 mg/mL (122 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years