For research use only. Not for therapeutic Use.
Vornorexant (ORN-0829; TS-142) is a potent dual OX1R and OX2R antagonist with IC50 values of 1.05 nM and 1.27 nM, respectively. Vornorexant exhibits potent sleep-promoting effects in vivo and can be used for insomnia research research.
Vornorexant (oral administration; 1-10 mg/kg) exhibits potent sleep-promoting effects at a po. dose of 1 mg/kg in a rat polysomnogram study. It results in a dose-dependent increase in the percentage of total sleep[1].Vornorexant exhibits optimal PK properties with a rapid Tmax and short half-lives in rats and dogs. The T1/2 is 0.238 hours and 1.16 hours, respectively in rat and dog[1].
| Catalog Number | I044386 |
| CAS Number | 1517965-94-4 |
| Synonyms | [(2S)-2-[[3-(5-fluoropyridin-2-yl)pyrazol-1-yl]methyl]-1,3-oxazinan-3-yl]-[5-methyl-2-(triazol-2-yl)phenyl]methanone |
| Molecular Formula | C23H22FN7O2 |
| Purity | ≥95% |
| InChI | InChI=1S/C23H22FN7O2/c1-16-3-6-21(31-26-8-9-27-31)18(13-16)23(32)30-10-2-12-33-22(30)15-29-11-7-20(28-29)19-5-4-17(24)14-25-19/h3-9,11,13-14,22H,2,10,12,15H2,1H3/t22-/m0/s1 |
| InChIKey | AEZZJXJIJFSUEM-QFIPXVFZSA-N |
| SMILES | CC1=CC(=C(C=C1)N2N=CC=N2)C(=O)N3CCCOC3CN4C=CC(=N4)C5=NC=C(C=C5)F |
| Reference | [1]. Aya Futamura, et al. Discovery of ORN0829, a potent dual orexin 1/2 receptor antagonist for the treatment of insomnia. Bioorg Med Chem. 2020 Jul 1;28(13):115489. |
