Bioactivity | 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 treatment research[1]. | ||||||||||||
In Vivo | 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]. Animal Model: | ||||||||||||
Name | Vornorexant | ||||||||||||
CAS | 1517965-94-4 | ||||||||||||
Formula | C23H22FN7O2 | ||||||||||||
Molar Mass | 447.46 | ||||||||||||
Appearance | Solid | ||||||||||||
Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
Storage |
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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. |