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Almorexant (hydrochloride)

Product Specifications

UNSPSC Description

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].

Target Antigen

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

Purity

99.98

Solubility

DMSO : ≥ 46 mg/mL|H2O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C)

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 Weight

549.02

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.bioRxiv. 2023 Jul 19.|Cell Metab. 2018 Jul 3;28(1):118-129.e5.|Nat Neurosci. 2024 Aug 6.|Oncotarget. 2018 Jan 9;9(6):6952-6967.

Shipping Conditions

Room Temperature

Storage Conditions

4°C (Powder, sealed storage, away from moisture)

Product Datasheet

http://file.medchemexpress.com/batch_PDF/HY-10805A/Almorexant-hydrochloride-DataSheet-MedChemExpress.pdf

Product MSDS

http://file.medchemexpress.com/batch_PDF/HY-10805A/Almorexant-hydrochloride-SDS-MedChemExpress.pdf

Clinical Information

Phase 3

CAS Number

913358-93-7

Available Sizes

Curated Selection

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