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Almorexant
$57 – $1,100
Products Details
Product 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].
Web ID
– HY-10805
Storage Temperature
– -20°C, 3 years; 4°C, 2 years (Powder)
Shipping
– Room Temperature
Applications
– Neuroscience-Neuromodulation
Molecular Formula
– C29H31F3N2O3
Citations
– Oncotarget. 2018 Jan 9;9(6):6952-6967. |bioRxiv. 2023 Jul 19.|Cell Metab. 2018 Jul 3;28(1):118-129.e5.
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.|[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.
CAS Number
– 871224-64-5
Molecular Weight
– 512.56
Compound Purity
– 99.71
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
Clinical Information
– Phase 3
Research Area
– Cancer; Endocrinology; Neurological Disease
Solubility
– DMSO : ≥ 46 mg/mL
Target
– Apoptosis;Calcium Channel;Caspase;Orexin Receptor (OX Receptor)
Isoform
– Calcium Channel;Caspase 3;OX1 Receptor;OX2 Receptor
Pathway
– Apoptosis;GPCR/G Protein;Membrane Transporter/Ion Channel;Neuronal Signaling
Product type
– Reference compound
Disclaimer: All products are for research use only unless clearly stated otherwise on the product datasheet. Datasheets provided on the website are drafts for reference purpose only and you are requested to always refer to the hard copy included in the kit for your experimentation.
