Cayman Filorexant

Filorexant is a dual antagonist of orexin 1 receptor (OX1R) and OX2R (K_is = 2.5 and 0.31 nM, respectively, for the recombinant human receptors).¹ It selectively inhibits OX1R and OX2R over a panel of more than 170 receptors and enzymes. Filorexant inhibits orexin A-induced calcium mobilization in CHO Cells expressing recombinant human OX1R or OX2R (K_b = 11 nM for both). It decreases locomotor activity in rats during the dark cycle when administered at a dose of 10 mg/kg. Filorexant (0.5 mg/kg) reduces the time spent awake and decreases the latency to slow-wave sleep stage 1 (SWS1) and SWS2, but not rapid eye movement (REM) sleep, in dogs. It increases the duration of SWS2, but not SWS1 or REM sleep, in the same model.

WARNING This product is not for human or veterinary use.