| Identification | Back Directory | [Name]
MK 6096 | [CAS]
1088991-73-4 | [Synonyms]
MK6096
MK-6096
MK 6096
CS-1825
Filorexant
MK 6096;MK6096
MK-6096(Filorexant)
Filorexant(MK-6096)
filorexant / MK-6096, CID25128145
[(2R,5R)-5-[(5-FLUOROPYRIDIN-2-YL)OXYMETHYL]-2-METHYLPIPERIDIN-1-YL]-(5-METHYL-2-PYRIMIDIN-2-YLPHENYL)METHANONE
[(2R,5R)-5-[[(5-Fluoro-2-pyridinyl)oxy]methyl]-2-methyl-1-piperidinyl][5-methyl-2-(2-pyrimidinyl)phenyl]methanone
Methanone, [(2R,5R)-5-[[(5-fluoro-2-pyridinyl)oxy]methyl]-2-methyl-1-piperidinyl][5-methyl-2-(2-pyrimidinyl)phenyl]-
((2R,5R)-5-(((5-Fluoropyridin-2-yl)oxy)methyl)-2-methylpiperidin-1-yl)(5-methyl-2-(pyrimidin-2-yl)phenyl)methanone MK6096 | [Molecular Formula]
C24H25FN4O2 | [MDL Number]
MFCD28100674 | [MOL File]
1088991-73-4.mol | [Molecular Weight]
420.48 |
| Chemical Properties | Back Directory | [Boiling point ]
540.2±50.0 °C(Predicted) | [density ]
1.203±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMF: 10mg/mL; DMF:PBS (pH 7.2) (1:4): 0.2mg/mL; DMSO: 2mg/mL; Ethanol: 5mg/mL | [form ]
A solid | [pka]
1.54±0.22(Predicted) | [color ]
Off-white to brown |
| Hazard Information | Back Directory | [Description]
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. | [Uses]
Filorexant is a selective dual orexin receptor antagonist with potent sleep-promoting properties. It has advanced into phase II clinical trials for the treatment of insomnia. | [in vivo]
Filorexant (MK-6096) dose-dependently reduced locomotor activity and significantly increased sleep in rats (3-30 mg/kg) and dogs (0.25 and 0.5 mg/kg). | [storage]
Store at -20°C | [References]
[1] CHRISTOPHER J. WINROW . Pharmacological characterization of MK-6096 – A dual orexin receptor antagonist for insomnia[J]. Neuropharmacology, 2012, 62 2: Pages 978-987. DOI: 10.1016/j.neuropharm.2011.10.003 |
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| Company Name: |
SPIRO PHARMA
|
| Tel: |
|
| Website: |
www.spiropharma.com.cn |
| Company Name: |
Musechem
|
| Tel: |
+1-800-259-7612 |
| Website: |
www.musechem.com |
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