Vornorexant (ORN-0829; TS-142) is a potent dual OX1R and OX2R antagonist with IC 50 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.
性状
Solid
体内研究(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.Vornorexant exhibits optimal PK properties with a rapid T max and short half-lives in rats and dogs. The T 1/2 is 0.238 hours and 1.16 hours, respectively in rat and dog. 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
Powder -20°C 3 years;4°C 2 years
ClinicalTrial
参考文献
[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.