Vornorexant (ORN-0829; TS-142) 是一种有效的 OX1R 和 OX2R 双拮抗剂，IC50 值分别为 1.05 nM 和 1.27 nM。Vornorexant 在动物模型中表现出有效的睡眠促进作用，可作用于治疗失眠。
货号:ajcx38372
CAS:1517965-94-4
分子式:C23H22FN7O2
分子量：447.46
溶解度:N/A
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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].

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].

[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.