Oveporexton  (Synonyms: TAK-861)

Oveporexton (TAK-861) is an orally active and selective OX2R agonist with an EC₅₀ of 2.5 nM. Oveporexton ameliorates narcolepsy-like phenotypes^[1][2].

Oveporexton potently activates recombinant OX2R (EC₅₀ of 2.5 nM) and weakly activates OX1R (EC₅₀ of 7500 nM)^[2].
Oveporexton (10-1000 nM) induces dose-dependent depolarization of the membrane potential in histaminergic neurons in the mouse tuberomammillary nucleus with an EC₅₀ of 31.7 nM^[2].

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

Oveporexton (0.03-10 mg/kg; p.o.) improves narcolepsy-like phenotype in mice, significantly increasing total waking time^[2].
Oveporexton (1 mg/kg; p.o.) significantly increases wakefulness time in cynomolgus monkeys^[2].

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

520.51

C₂₃H₂₅F₅N₂O₄S

2460722-04-5

CC(C)(O)C(N(CC(F)([C@@H]1NS(CC)(=O)=O)F)[C@H]1CC2=C(C(C3=CC(F)=CC(F)=C3)=CC=C2)F)=O

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. International Nonproprietary Names for Pharmaceutical Substances (INN). WHO Drug Information, Vol. 38, No. 2, 2024.

  [2]. Mitsukawa K, et al. TAK-861, a potent, orally available orexin receptor 2-selective agonist, produces wakefulness in monkeys and improves narcolepsy-like phenotypes in mouse models. Sci Rep. 2024 Sep 6;14(1):20838.  [Content Brief]