Seltorexant 是一种可口服，高亲和性以及选择性的 orexin-2 受体(OX2R)拮抗剂，对人和大鼠中的 OX2R 的pKi值分别为 8.0 和 8.1。它穿过血脑屏障，迅速占据大鼠大脑中的 OX2R 结合位点。
产品描述
Seltorexant 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).
体内活性
Seltorexant (3-30 mg/kg; p.o.) dose-dependently causes and prolongs sleep in male Sprague-Dawley rats. The sleep-promoting effects of Seltorexant (30 mg/kg; p.o.; per day for 7 days) are maintained upon 7-day repeated dosing in rats [1].
Cas No.
1293281-49-8
分子式
C21H22FN7O
分子量
407.44
别名
JNJ-42847922
储存和溶解度
DMSO:250 mg/mL (613.59 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years
