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