mk-1064

MK‑1064 is an orally bioavailable, selective orexin 2 receptor (OX2R) antagonist developed by Merck for the treatment of insomnia and sleep disorders. It acts as a small molecule that selectively blocks the orexin type 2 receptor with high affinity (Ki ≈0.52 nM), showing over a thousand-fold selectivity versus orexin type 1 receptor. Preclinical studies demonstrated that MK‑1064 promotes both REM and non‑REM sleep in animal models and healthy human subjects by attenuating arousal and increasing total sleep time. Clinical trials have evaluated its safety, pharmacokinetics, and pharmacodynamics in healthy volunteers; however, it has not been approved for any indication to date[1][3][5][8].

Other names

1207253-08-45''-chloro-N-[(5,6-dimethoxypyridin-2-yl)methyl]-2,2':5',3''-terpyridine-3'-carboxamide5-(5-chloropyridin-3-yl)-N-[(5,6-dimethoxypyridin-2 yl)methyl]-2-pyridin 2 yl pyridine 3 carboxamide