Tasimelteon

＞98%

Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.

他司美琼；BMS-214778；VEC-162

DMSO ≥33 mg/mL

MT2 receptor ,MT1 receptor

Tasimelteon is a circadian regulator that resets the master clock in the suprachiasmatic nuclei of the hypothalamus by binding to both melatonin MT1 and MT2 receptors making it a dual melatonin receptor agonist. The affinity of tasimelteon for the MT2 receptor is 4-fold higher than its affinity for the MT1 receptor.

In rats and monkeys, the half-life of tasimelteon was approximately 2 h which is longer than the half-life of melatonin. Tasimelteon has a mean absolute bioavailability of approximately 38.3%. The higher oral-to-IV exposure ratios and decrease in the metabolite-to-parent ratios after IV administration for tasimelteon's metabolites indicate that although tasimelteon is subject to first-pass metabolism, a substantial fraction of its metabolism occurs post- rather than presystemically. Both oral and IV tasimelteon were well tolerated.