| Description | Seltorexant (JNJ-42847922) crosses the blood-brain barrier and quickly occupies OX2R binding sites in the rat brain. Seltorexant is a high-affinity and selective orexin-2 receptor antagonist (pKi: 8.0 and 8.1 for human and rat OX2R). |
| In vivo | Seltorexant（口服 3-30 mg/kg）能够剂量依赖性地诱发并延长雄性Sprague-Dawley大鼠的睡眠时间。连续七天每天给药（口服，30 mg/kg）后， Seltorexant 的促睡眠效果在大鼠体内得以保持[1]。 |
| Target activity | OX2:8.0 (pki)(human), OX2:8.1 (pki)(rat) |
| Synonyms | JNJ-42847922 |
| molecular weight | 407.44 |
| Molecular formula | C21H22FN7O |
| CAS | 1293281-49-8 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 250 mg/mL (613.59 mM), Sonication is recommended. |
| References | 1. Bonaventure P, et al. Characterization of JNJ-42847922, a Selective Orexin-2 Receptor Antagonist, as a Clinical Candidate for the Treatment of Insomnia. J Pharmacol Exp Ther. 2015 Sep;354(3):471-82. |