Almorexant (hydrochloride)

Almorexant (ACT 078573) hydrochloride 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 hydrochloride reversibly blocks signaling of orexin-A and orexin-B peptides. Almorexant hydrochloride totally blocked the intracellular Ca2+ signal pathway. Almorexant hydrochloride stimulates caspase-3 activity in AsPC-1 cells and induces apoptosis[1][2][3][4].

Product Specifications

CAS Number

[913358-93-7]

Product Name Alternative

ACT 078573 hydrochloride

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

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-hydrochloride.html

Concentration

10mM

Purity

99.98

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.Cl

Molecular Formula

C29H32ClF3N2O3

Molecular Weight

549.02

Precautions

H302, H315, H319, H335

References & Citations

[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.|[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.|[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.|[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.