Seltorexant

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效的、选择性的、口服活性的 orexin-2 受体 (OX2R) 拮抗剂，对人和大鼠 OX2R 的 pKi 分别为 8.0 和 8.1。

A potent, selective, orally active orexin-2 receptor (OX2R) antagonist with pKi of 8.0 and 8.1 for human and rat OX2R, respectively; displays an 2-log selectivity over OX1R, and shows no significant affinity for 50 receptor/transporter/ion channel (<50% inhibition at 1 uM); reduces the latency to non–rapid eye movement (NREM) sleep and prolongs NREM sleep time in rats (3–30 mg/kg).Sleep Disorder Phase 2 Clinical(In Vivo):Seltorexant (JNJ-42847922) (3-30 mg/kg; p.o.) dose-dependently induces and prolongs sleep in male Sprague-Dawley rats.The sleep-promoting effects of JNJ-42847922 (30 mg/kg; p.o.; per day for 7 days) are maintained upon 7-day repeated dosing in rats.

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Animal Model:Male Sprague-Dawley rats (350-450 g)Dosage:30 mg/kg Administration:p.o.; per day for 7 daysResult:The reduced sleep onset (non–rapid eye movement (NREM) latency) and the increased NREM sleep duration were maintained upon 7-day repeated dosing with JNJ-42847922. The prolongation of NREM sleep time was due to a significant increase in NREM bout duration throughout the treatment period assessed on D1 and D7. Rapid eye movement (REM) sleep was only marginally affected on D4 of treatment, resulting in a small but significant reduction in REM sleep latency and an increase in REM sleep duration.

MIN-202 | JNJ-42847922 | JNJ-922

GPCR/G Protein

Orexin Receptor

Orexin Receptor

Neurological Disease

Sleep Disorder

1293281-49-8

407.453

C21H22FN7O

>98% (HPLC)

In Vitro:?DMSO : 25 mg/mL (61.36 mM)

O=C(N1C[C@@](CN(C2=NC(C)=CC(C)=N2)C3)([H])[C@@]3([H])C1)C4=C(N5N=CC=N5)C=CC=C4F

((3aR,6aS)-5-(4,6-dimethylpyrimidin-2-yl)hexahydropyrrolo[3,4-c]pyrrol-2(1H)-yl)(2-fluoro-6-(2H-1,2,3-triazol-2-yl)phenyl)methanone

(-20℃)

With Ice Pack

≥ 2 years