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Almorexant hydrochloride Data Sheet
| Product Name: | Almorexant hydrochloride |
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|---|---|---|
| CAS No.: | 913358-93-7 | |
| Cat. No.: | HY-10805A | |
| MWt: | 549.02 | |
| Formula: | C29H32ClF3N2O3 | |
| Purity : | >98% | |
| Solubility: | DMSO : ≥ 46 mg/mL;H<sub>2</sub>O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) | |
| Mechanisms: | Target: Cancer Endocrinology Neurological Disease | |
| Biological Activity: | ||
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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].
IC50 & Target: Kd: 0.17 nM (hOX2), 1.3 nM (hOX1)[2]
In Vitro: Almorexant hydrochloride (1 μM) promote tyrosine phosphorylation of SHP2/OX1R complex[1]. Almorexant hydrochloride (1 μM) inhibits the cellular growth of AsPC-1 cells[1]. In Vivo: Almorexant hydrochloride (1.8 μmol/kg, 100 μL; IP, daily) reduces the volume of tumors[2]. Almorexant hydrochloride (300 mg/kg, PO, once) can help rats to be fully capable of spatial and avoidance learning[4]. Almorexant hydrochloride (30-300 mg/kg) dose-dependently increases rapid eye movement (REM) and non-REM (NREM) sleep and decreases wakefulness apparently without inducing either cataplexy18 or deficits in next-day performance[3]. |
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