CAS No. : 1088991-73-4

Product Details
For research use only. Not Intended for Therapeutic Use!
Cat No:I000376
Molecular Formula:C24H25FN4O2
Molecular Weight:420.48
Target:Orexin receptor antagonist
IC50:< 3 nM(binding Ki) [1]
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Appearance:Solid powder
Purity: > 98%
Cat No:I000376
Cas No:1088991-73-4

MK-6096(Filorexant) is an orally bioavailable potent and selective reversible antagonist of OX1 and OX2 receptor(<3 nM in binding).
IC50 value: < 3 nM(binding Ki) [1]
Target: Orexin receptor antagonist
in vitro: In radioligand binding and functional cell based assays 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.
in vivo: 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).

1:A Phase II Dose-Ranging Study Evaluating the Efficacy and Safety of the Orexin Receptor Antagonist Filorexant (MK-6096) in Patients with Primary Insomnia. Connor KM, Mahoney E, Jackson S, Hutzelmann J, Zhao X, Jia N, Snyder E, Snavely D, Michelson D, Roth T, Herring WJ.Int J Neuropsychopharmacol. 2016 Aug 12;19(8). pii: pyw022. doi: 10.1093/ijnp/pyw022. Print 2016 Aug. PMID: 26979830 Free PMC Article
2:Unusual pyrimidine participation: efficient stereoselective synthesis of potent dual orexin receptor antagonist MK-6096. Chung JY, Zhong YL, Maloney KM, Reamer RA, Moore JC, Strotman H, Kalinin A, Feng R, Strotman NA, Xiang B, Yasuda N.Org Lett. 2014 Nov 21;16(22):5890-3. doi: 10.1021/ol5028249. Epub 2014 Nov 3. PMID: 25365229
3:Discovery of [(2R,5R)-5-{[(5-fluoropyridin-2-yl)oxy]methyl}-2-methylpiperidin-1-yl][5-methyl-2-(pyrimidin-2-yl)phenyl]methanone (MK-6096): a dual orexin receptor antagonist with potent sleep-promoting properties. Coleman PJ, Schreier JD, Cox CD, Breslin MJ, Whitman DB, Bogusky MJ, McGaughey GB, Bednar RA, Lemaire W, Doran SM, Fox SV, Garson SL, Gotter AL, Harrell CM, Reiss DR, Cabalu TD, Cui D, Prueksaritanont T, Stevens J, Tannenbaum PL, Ball RG, Stellabott J, Young SD, Hartman GD, Winrow CJ, Renger JJ.ChemMedChem. 2012 Mar 5;7(3):415-24, 337. doi: 10.1002/cmdc.201200025. Epub 2012 Feb 3. PMID: 22307992
4:Pharmacological characterization of MK-6096 - a dual orexin receptor antagonist for insomnia. Winrow CJ, Gotter AL, Cox CD, Tannenbaum PL, Garson SL, Doran SM, Breslin MJ, Schreier JD, Fox SV, Harrell CM, Stevens J, Reiss DR, Cui D, Coleman PJ, Renger JJ.Neuropharmacology. 2012 Feb;62(2):978-87. doi: 10.1016/j.neuropharm.2011.10.003. Epub 2011 Oct 18. PMID: 22019562
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