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Seltorexant

Chemical Structure : Seltorexant

CAS No.: 1293281-49-8

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

Catalog No.: PC-61107Not For Human Use, Lab Use Only.

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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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

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

Sleep Disorder

Phase 2 Clinical

Physicochemical Properties

M.Wt 407.453
Formula C21H22FN7O
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
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

References

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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