JNJ-54717793 是一种具有口服活性、脑穿透性、选择性和高亲和力的orexin-1 receptor(OX1R) 拮抗剂(血浆EC50=85 ng/mL)。JNJ-54717793 的 hOX1R 和 hOX2RKi值分别为 16 nM 和 700 nM。JNJ-54717793 是一种有效的焦虑症化合物。

JNJ-54717793 is an orally active, brain penetrating, selective and high affinity orexin-1 receptor (OX1R) antagonist (plasma EC 50 =85 ng/mL). The K i values of JNJ-54717793 for hOX1R (human OX1R) and hOX2R are 16 nM and 700 nM, respectively. JNJ-54717793 is a potent compound of anxiety disorders [1] [2].

JNJ-5471779 (30 mg/kg; p.o.; 6 hours) significantly reduces the latency for rapid eye movement (REM) sleep and increases the time spent in REM sleep [2]. JNJ-5471779 (3~30 mg/kg; p.o.) attenuates bradycardia responses [2]. JNJ-5471779 (5mg/kg; p.o.) shows low clearance [1]. Animal Model: OX2R KO mice [2] Dosage: 30 mg/kg Administration: P.o. Result: Significantly reduced the latency for rapid eye movement (REM) sleep and prolonged the time spent in REM sleep. Animal Model: Rat [2] Dosage: 3~30 mg/kg Administration: P.o. Result: Attenuated bradycardia responses. Animal Model: Mouse [1] Dosage: 5.0 mg/kg (Pharmacokinetic Analysis) Administration: P.o. Result: Clearance was found to be low.

1628843-99-1

C22H18F4N6O

458.41

JNJ-54717793

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years