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Almorexant HCl(ACT 078573)
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 HCl(ACT 078573)图片
CAS NO:913358-93-7
规格:≥98%
包装与价格:
包装价格(元)
2mg电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)549.02
FormulaC29H32ClF3N2O3
CAS No.913358-93-7 (HCl salt);
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 72 mg/mL (131.1 mM)
Water: <1 mg/mL
Ethanol: 51 mg/mL (92.9 mM)
Solubility (In vivo)2% DMSO+25% β-cyclodextrin+saline: 9 mg/mL
SynonymsACT078573 HCl; ACT-078573 HCl; Almorexant HCl; ACT 078573 HCl;
实验参考方法
In Vitro

In vitro activity: 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.


Kinase Assay: In binding kinetic analyses, [(3)H]almorexant had fast association and dissociation rates at hOX(1), whereas it had a fast association rate and a remarkably slow dissociation rate at hOX(2).


Cell Assay: Almorexant (also known as ACT078573) is a novel, potent, orally bioactive, competitive and dual orexin receptor antagonist with IC50 of 6.6 nM and 3.4 nM for OX1 and OX2 receptor, respectively. It has the potential for treating insomnia. In the inositol phosphates assay, almorexant acts as a competitive antagonist of hOX1R but a noncompetitive-like antagonist of hOX2R. Furthermore, almorexant shows effects on sleep in multiple species, including man.

In VivoAlmorexant (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.
Animal modelWistar rats.
Formulation & DosageDissolved in Polyethylene glycol (PEG) 400 or 0.25% methylcellulose in water; 300 mg/kg; p.o. administration
ReferencesNat Med. 2007 Feb;13(2):150-5; Neuropsychopharmacology. 2012 Sep;37(10):2210-21; Front Neurosci. 2014 Feb 25;8:33.