Seltorexant hydrochloride (Synonyms: JNJ-42847922 hydrochloride)
目录号: PL08096 纯度: ≥99%
CAS No. :1293284-49-7
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中文名称
Seltorexant hydrochloride
英文名称
Seltorexant hydrochloride
英文别名
Seltorexant hydrochloride;Seltorexant (hydrochloride);[2-(4,6-dimethylpyrimidin-2-yl)-1,3,3a,4,6,6a-hexahydropyrrolo[3,4-c]pyrrol-5-yl]-[2-fluoro-6-(triazol-2-yl)phenyl]methanone;hydrochloride
Cas No.
1293284-49-7
分子式
C21H23ClFN7O
分子量
443.91
包装储存
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
产品详情
Seltorexant hydrochloride (JNJ-42847922 hydrochloride) 是一种具有口服活性的,高亲和性以及选择性的 OX2R 拮抗剂 (人和大鼠中的 OX2R 的pKi 值分别为 8.0 和 8.1)。Seltorexant hydrochloride 穿过血脑屏障,迅速占据大鼠大脑中的 OX2R 结合位点。
生物活性
Seltorexant hydrochloride (JNJ-42847922 hydrochloride) is an orally active, high-affinity, and selective OX2R antagonist (pK i values of 8.0 and 8.1 for human and rat OX2R). Seltorexant hydrochloride crosses the blood-brain barrier and quickly occupies OX2R binding sites in the rat brain.
性状
Solid
IC50 & Target[1][2]
human OX2R 8.0 (pKi) rat OX2R 8.1 (pKi)
体内研究(In Vivo)
Seltorexant hydrochloride (JNJ-42847922 hydrochloride) (3-30 mg/kg; p.o.) dose-dependently induces and prolongs sleep in male Sprague-Dawley rats.
The sleep-promoting effects of Seltorexant hydrochloride (30 mg/kg; p.o.; per day for 7 days) are maintained upon 7-day repeated dosing in rats. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
ClinicalTrial
参考文献
[1]. Bonaventure P, et al. Characterization of JNJ-42847922, a Selective Orexin-2 Receptor Antagonist, as a Clinical Candidate for the Treatment of Insomnia. J Pharmacol Exp Ther. 2015 Sep;354(3):471-82.
溶解度数据
In Vitro: H2O : 100 mg/mL (225.27 mM; Need ultrasonic)DMSO : 83.33 mg/mL (187.72 mM; Need ultrasonic)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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