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JNJ-54717793
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
JNJ-54717793图片
CAS NO:1628843-99-1
包装与价格:
包装价格(元)
5mg电议
10mg电议

产品介绍
JNJ-54717793 作为脑渗透剂,是一种具有口服活性、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 hOX2R Ki值分别为 16 nM 和 700 nM。JNJ-54717793 是焦虑症的有效化合物。
Cas No.1628843-99-1
分子式C22H18F4N6O
分子量458.41
溶解度DMSO : 240 mg/mL (523.55 mM; Need ultrasonic)
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

JNJ-54717793, as a brain penetrant, is an orally active, selective and high affinity orexin-1 receptor (OX1R) antagonist (plasma EC50=85 ng/mL). The Ki 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 prolongs 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].

[1]. PrÉville C, et al. Substituted Azabicyclo[2.2.1]heptanes as Selective Orexin-1 Antagonists: Discovery of JNJ-54717793. ACS Med Chem Lett. 2020;11(10):2002-2009. Published 2020 Apr 27.
[2]. Bonaventure P, et al. Evaluation of JNJ-54717793 a Novel Brain Penetrant Selective Orexin 1 Receptor Antagonist in Two Rat Models of Panic Attack Provocation. Front Pharmacol. 2017;8:357. Published 2017 Jun 9.