Almorexant
Product Specifications
UNSPSC 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[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.html
Purity
99.71
Solubility
DMSO : ≥ 46 mg/mL
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 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.Oncotarget. 2018 Jan 9;9(6):6952-6967. |bioRxiv. 2023 Jul 19.|Cell Metab. 2018 Jul 3;28(1):118-129.e5.|Nat Neurosci. 2024 Aug 6.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Product Datasheet
http://file.medchemexpress.com/batch_PDF/HY-10805/Almorexant-DataSheet-MedChemExpress.pdf
Product MSDS
http://file.medchemexpress.com/batch_PDF/HY-10805/Almorexant-SDS-MedChemExpress.pdf
Clinical Information
Phase 3
CAS Number
871224-64-5
Available Sizes
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