Firazorexton hydrate  (Synonyms: TAK-994)

Firazorexton hydrate (TAK-994) is an orally active and brain-penetrant orexin type 2 receptor (OX2R) selective agonist. Firazorexton hydrate can promote wakefulness and has the potential to improve narcolepsy-like symptoms in mice^[1].

Firazorexton (hydrate) (1-1000 nM) 以剂量依赖性的方式增加 hOX2R/CHO-K1 细胞中的钙动员，EC₅₀ 为 19 nM^[1]。
Firazorexton (hydrate) (1 nM-10 μM) 在 hOX2R/CHO-EA 细胞中激活 OX2R 下游信号，增加 β-arrestin 的招募 (EC₅₀ : 100 nM)，诱导 ERK1/2 的磷酸化 (EC₅₀ : 170 nM)^[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Firazorexton (hydrate) (口服; 30 mg/kg; 单剂量 ) 可增加 C57BL/6J 小鼠的总觉醒时间^[1]。
Firazorexton (hydrate) (口服; 3-10 mg/kg; 单剂量) 可改善嗜睡症小鼠模型中发作性睡病样症状^[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

497.53

C₂₂H₂₅F₃N₂O₄S.3/2H₂O

2861934-86-1

固体

White to off-white

Room temperature in continental US; may vary elsewhere.

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

• [1]. Ishikawa T, et al. TAK-994, a Novel Orally Available Brain-Penetrant Orexin 2 Receptor-Selective Agonist, Suppresses Fragmentation of Wakefulness and Cataplexy-Like Episodes in Mouse Models of Narcolepsy. J Pharmacol Exp Ther. 2023 Jun;385(3):193-204.  [Content Brief]