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首页-小分子抑制剂&激动剂-GPCR-Orexin Receptor-Seltorexant
Seltorexant

Chemical Structure : Seltorexant

CAS No.: 1293281-49-8

Seltorexant (MIN-202, JNJ-42847922, JNJ-922)

货号: PC-61107Not For Human Use, Lab Use Only.

Seltorexant (JNJ-42847922, MIN-202) is a potent, selective, orally active orexin-2 receptor (OX2R) antagonist with pKi of 8.0 and 8.1 for human and rat OX2R, respectively.

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10 mg ¥1280 In stock
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50 mg ¥2980 In stock
100 mg ¥4280 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Seltorexant (JNJ-42847922, MIN-202) is a potent, selective, orally active orexin-2 receptor (OX2R) antagonist with pKi of 8.0 and 8.1 for human and rat OX2R, respectively.
Seltorexant displays an 2-log selectivity over OX1R, and shows no significant affinity for 50 receptor/transporter/ion channel (<50% inhibition at 1 uM).
Seltorexant reduces the latency to non–rapid eye movement (NREM) sleep and prolongs NREM sleep time in rats (3–30 mg/kg).

物理化学性质&存储条件

分子量 407.453
分子式 C21H22FN7O
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

((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

参考文献

1. Letavic MA, et al. J Med Chem. 2015 Jul 23;58(14):5620-36.

2. Bonaventure P, et al. J Pharmacol Exp Ther. 2015 Sep;354(3):471-82.

3. Yun S, et al. Front Behav Neurosci. 2017 May 8;11:83.

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