Almorexant
CAS No. : 871224-64-5
(Synonyms: ACT 078573)
| Size | Price | Stock |
|---|---|---|
| 5mg | $111 | In-stock |
| 10mg | $178 | In-stock |
| 25mg | $416 | In-stock |
| 50mg | $666 | In-stock |
| 100mg | $1000 | In-stock |
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| Cat. No. : | HY-10805 |
| M.Wt: | 512.56 |
| Formula: | C29H31F3N2O3 |
| Purity: | >98 % |
| Solubility: | DMSO : ≥ 46 mg/mL |
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].
IC50 & Target: Kd: 0.17 nM (hOX2), 1.3 nM (hOX1)[2]
In Vitro: Almorexant (1 μM) promotes tyrosine phosphorylation of SHP2/OX1R complex[1].
Almorexant (1 μM) inhibits the cellular growth of AsPC-1 cells[1].
In Vivo: Almorexant (1.8 μmol/kg, 100 μL; IP, daily) reduces the volume of tumors[2].
Almorexant (300 mg/kg, PO, once) can help rats to be fully capable of spatial and avoidance learning[4].
Almorexant (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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