Filorexant
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).
| Supplier | Ace Therapeutics |
|---|---|
| Product # | SMD1292 |
| CAS # | 1088991-73-4 |
| Pricing | Customizable size, Inquiry |
| Synonym | MK6096; MK-6096; MK 6096; Filorexant |
| Product Category | Lab-use Small Molecule Drugs |
| Chemical Formula | C24H25FN4O2 |
| Exact Mass | 420.1962 |
| Molecular Weight | 420.4884 |
| Elemental Analysis | C, 68.55; H, 5.99; F, 4.52; N, 13.32; O, 7.61 |
| 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 |
| Appearance | Solid powder |
| 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 |
| Availability | 2 Weeks |