Related Diseases
                                                                Insomnia
                             
                                                                                                                    
                                                                                                                    
                                                                        
                                                                        
                                                                        
                                                                Description
                                                                Filorexant, also known as MK6096, is an orally bioavailable potent and selective reversible antagonist of OX(1)R and OX(2)R currently in clinical development for insomnia. MK-6096 demonstrated potent binding and antagonism of both human OX(1)R and OX(2)R (<3 nM in binding, 11 nM in FLIPR), with no significant off-target activities against a panel of >170 receptors and enzymes. MK-6096 occupies 90% of human OX(2)Rs expressed in transgenic rats at a plasma concentration of 142 nM, and dose-dependently reduced locomotor activity and significantly increased sleep in rats (3-30 mg/kg) and dogs (0.25 and 0.5 mg/kg).
                             
                                                                        
                                                                        
                                                                Chemical Formula
                                                                C24H25FN4O2
                             
                                                                        
                                                                        
                                                                Molecular Weight
                                                                420.4884
                             
                                                                        
                                                                Elemental Analysis
                                                                C, 68.55; H, 5.99; F, 4.52; N, 13.32; O, 7.61
                             
                                                                        
                                                                Synonym
                                                                MK6096; MK-6096; MK 6096; Filorexant
                             
                                                                        
                                                                IUPAC/Chemical Name
                                                                ((2R,5R)-5-(((5-fluoropyridin-2-yl)oxy)methyl)-2-methylpiperidin-1-yl)(5-methyl-2-(pyrimidin-2-yl)phenyl)methanone
                             
                                                                        
                                                                InChi Key
                                                                NPFDWHQSDBWQLH-QZTJIDSGSA-N
                             
                                                                        
                                                                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
                             
                                                                        
                                                                SMILES Code
                                                                O=C(N1[C@H](C)CC[C@@H](COC2=NC=C(F)C=C2)C1)C3=CC(C)=CC=C3C4=NC=CC=N4
                             
                                                                        
                                                                        
                                                                Purity
                                                                >98% (or refer to the Certificate of Analysis)
                             
                                                                        
                                                                Shipping Condition
                                                                Shipped under ambient temperature as non-hazardous chemical.  This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
                             
                                                                        
                                                                Storage Condition
                                                                Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
                             
                                                                        
                                                                Solubility
                                                                Soluble in DMSO, not in water
                             
                                                                        
                                                                Shelf Life
                                                                >2 years if stored properly
                             
                                                                        
                                                                Drug Formulation
                                                                This drug may be formulated in DMSO
                             
                                                                        
                                                                Stock Solution Storage
                                                                0 - 4℃ for short term (days to weeks), or -20℃ for long term (months).
                             
                                                                        
                                                                HS Tariff Code
                                                                2934.99.9001