MedChemExpress - Model Almorexant -871224-64-5

Almorexant (ACT 078573) is an orally active, potent and competitive dual orexin receptor antagonist, with Kd values of 1.3 nM (OX1) and 0.17 nM (OX2), respectively. Almorexant reversibly blocks signaling of orexin-A and orexin-B peptides. Almorexant totally blocked the intracellular Ca2+ signal pathway. Almorexant stimulates caspase-3 activity in AsPC-1 cells and induces apoptosis[1][2][3][4].

Almorexant

MCE China：Almorexant

Brand：MedChemExpress (MCE)

Cat. No.HY-10805

CAS：871224-64-5

Synonyms：ACT 078573

Purity：99.71%

Storage：Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year

Shipping：Room temperature in continental US; may vary elsewhere.

Description：Almorexant (ACT 078573) is an orally active, potent and competitive dual orexin receptor antagonist, with Kd values of 1.3 nM (OX1) and 0.17 nM (OX2), respectively. Almorexant reversibly blocks signaling of orexin-A and orexin-B peptides. Almorexant totally blocked the intracellular Ca2+ signal pathway. Almorexant stimulates caspase-3 activity in AsPC-1 cells and induces apoptosis.

In Vitro：Almorexant (1 μM) promotes tyrosine phosphorylation of SHP2/OX1R complex[1]. Almorexant (1 μM) inhibits the cellular growth of AsPC-1 cells[1].

In Vivo：Almorexant (1.8 μmol/kg, 100 μL; IP, daily) reduces the volume of tumors[2]. Almorexant (300 mg/kg, PO, once) can help rats to be fully capable of spatial and avoidance learning[4]. Almorexant (30-300 mg/kg) dose-dependently increases rapid eye movement (REM) and non-REM (NREM) sleep and decreases wakefulness apparently without inducing either cataplexy18 or deficits in next-day performance[3].

IC50 & Target：human OX2R 0.17 nM (Kd) human OX1R 1.3 nM (Kd) Caspase-3

References：

[1]. Dayot S, et al. In vitro, in vivo and ex vivo demonstration of the antitumoral role of hypocretin-1/orexin-A and almorexant in pancreatic ductal adenocarcinoma. Oncotarget. 2018 Jan 9;9(6):6952-6967. [Content Brief]

[2]. Malherbe P, et al. Biochemical and electrophysiological characterization of almorexant, a dual orexin 1 receptor (OX1)/orexin 2 receptor (OX2) antagonist: comparison with selective OX1 and OX2 antagonists. Mol Pharmacol. 2009 Sep;76(3):618-31. [Content Brief]

[3]. Black SW, et al. Almorexant promotes sleep and exacerbates cataplexy in a murine model of narcolepsy. Sleep. 2013 Mar 1;36(3):325-36. [Content Brief]

[4]. Dietrich H, et al. Intact learning and memory in rats following treatment with the dual orexin receptor antagonist almorexant. Psychopharmacology (Berl). 2010 Oct;212(2):145-54. [Content Brief]

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MedChemExpress - Model Almorexant -871224-64-5

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Almorexant