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) increases calcium mobilization in hOX2R/CHO-K1 cells in a dose-dependent manner, with an EC₅₀ of 19 nM^[1].
Firazorexton (hydrate) (1 nM-10 μM) activates downstream signals of OX2R, increases the recruitment of β-arrestin (EC₅₀: 100 nM), and induces the phosphorylation of ERK1/2 (EC₅₀: 170 nM) in hOX2R/CHO-EA cells^[1].

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

Firazorexton (hydrate) (oral administration; 30 mg/kg; single dose) can increase the total wakefulness time in C57BL/6J mice^[1].
Firazorexton (hydrate) (oral administration; 3-10 mg/kg; single dose) can improve narcolepsy-like symptoms in mouse models of narcolepsy^[1].

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

497.53

C₂₂H₂₅F₃N₂O₄S.3/2H₂O

2861934-86-1

Solid

White to off-white

O=C(N(CC1)[C@H]([C@H]1N[S](C)(=O)=O)CC(C=CC=C2C3=CC(F)=CC(F)=C3)=C2F)C(C)(O)C.[1.5].O

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]