Filorexant

Filorexant is a dual antagonist of orexin 1 receptor (OX1R) and OX2R (Kis = 2.5 and 0.31 nM, respectively, for the recombinant human receptors). 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 (Kb = 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.Formal Name: [(2R,5R)-5-[[(5-fluoro-2-pyridinyl)oxy]methyl]-2-methyl-1-piperidinyl][5-methyl-2-(2-pyrimidinyl)phenyl]-methanone. CAS Number: 1088991-73-4. Molecular Formula: C24H25FN4O2. Formula Weight: 420.5. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMF: 10mg/mL, DMF:PBS (pH 7.2) (1:4): 0.2mg/mL, DMSO: 2mg/mL, Ethanol: 5mg/mL. lambdamax: 268 nm. SMILES: FC1=CC=C(OC[C@H]2CN(C(C3=CC(C)=CC=C3C4=NC=CC=N4)=O)[C@H](C)CC2)N=C1. InChi Code: InChI=1S/C24H25FN4O2/c1-16-4-8-20(23-26-10-3-11-27-23)21(12-16)24(30)29-14-18(6-5-17(29)2)15-31-22-9-7-19(25)13-28-22/h3-4,7-13,17-18H,5-6,14-15H2,1-2H3/t17-,18-/m1/s1. InChi Key: NPFDWHQSDBWQLH-QZTJIDSGSA-N.