化合物 JNJ-54717793 T9654

Product Introduction
Bioactivity


英文名: JNJ-54717793

描述: 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。

体内活性: 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.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

关键字: JNJ54717793 | JNJ-54717793 | JNJ 54717793

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途