Seltorexant (JNJ-42847922) 是一种具有口服活性的，高亲和性以及选择性的 OX2R 拮抗剂 (人和大鼠中的 OX2R 的pKi 值分别为 8.0 和 8.1)。Seltorexant (JNJ-42847922) 穿过血脑屏障，迅速占据大鼠大脑中的 OX2R 结合位点。
CAS：1293281-49-8
分子式：C21H22FN7O
分子量：407.44
纯度：98%
存储：Store at -20°C

Background:

Seltorexant (JNJ-42847922) is an orally active, high-affinity, and selective OX2R antagonist (pKi values of 8.0 and 8.1 for human and rat OX2R). Seltorexant (JNJ-42847922) crosses the blood-brain barrier and quickly occupies OX2R binding sites in the rat brain[1]. pKi: 8.0 (human OX2R), 8.1 (rat OX2R)[1]

[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.