Almorexant

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].

Product Specifications

CAS Number

[871224-64-5]

Product Name Alternative

ACT 078573

UNSPSC

12352005

Target

Apoptosis; Calcium Channel; Caspase; Orexin Receptor (OX Receptor)

Type

Reference compound

Related Pathways

Apoptosis; GPCR/G Protein; Membrane Transporter/Ion Channel; Neuronal Signaling

Applications

Neuroscience-Neuromodulation

Field of Research

Cancer; Endocrinology; Neurological Disease

Assay Protocol

https://www.medchemexpress.com/almorexant.html

Purity

99.96

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

CNC([C@@H](C1=CC=CC=C1)N2CCC3=CC(OC)=C(OC)C=C3[C@@H]2CCC4=CC=C(C(F)(F)F)C=C4)=O

Molecular Formula

C29H31F3N2O3

Molecular Weight

512.56

References & Citations

[1]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.|[2]Black SW, et al. Almorexant promotes sleep and exacerbates cataplexy in a murine model of narcolepsy. Sleep. 2013 Mar 1;36 (3) :325-36.|[3]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.|[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.