| Description | ACT-462206 is an orally available Orexin 1/Orexin 2 receptor antagonist that crosses the blood-brain barrier.ACT-462206 is highly potent and can be used in studies of sleep and anxiety. |
| In vivo | 在雄性 Wistar 大鼠中，ACT-462206（0、10、30、100、300 mg/kg；口服灌胃；单次剂量）的结果显示，ACT-462206 降低了第一次非快速眼动睡眠的持续时间（60秒）和第一次快速眼动睡眠的持续时间（30秒）。并且 ACT-462206 以剂量依赖的方式降低了总觉醒时间和行为活动，同时增加了快速眼动睡眠和非快速眼动睡眠的时间[1]。 |
| molecular weight | 388.48 |
| Molecular formula | C20H24N2O4S |
| CAS | 1361321-96-1 |
| Storage | keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 80 mg/mL (205.93 mM), Sonication is recommended. |
| References | 1. Boss C, et al. Structure-activity relationship, biological, and pharmacological characterization of the proline sulfonamide ACT-462206: a potent, brain-penetrant dual orexin 1/orexin 2 receptor antagonist. ChemMedChem. 2014 Nov;9(11):2486-96. 2. Hoch M, van Gorsel H, van Gerven J, Dingemanse J. Entry-into-humans study with ACT-462206, a novel dual orexin receptor antagonist, comparing its pharmacodynamics with almorexant. J Clin Pharmacol. 2014 Sep;54(9):979-86. doi: 10.1002/jcph.297. PubMed PMID: 24691844. |