Name | Filorexant |
Description | Filorexant (MK-6096) is an orally bioavailable, effective, and selective reversible antagonist of OX1 and OX2 receptors, with (Ki <3 nM). |
In vitro | Filorexant occupies 90% of human OX(2)Rs expressed in transgenic rats at a plasma concentration of 142 nM. Filorexant demonstrated effective binding and antagonism of both human OX(1)R and OX(2)R (<3 nM in binding, 11 nM in FLIPR), in radioligand binding and functional cell-based assays. It has no significant off-target activities against a panel of >170 receptors and enzymes [1]. |
In vivo | Filorexant dose-dependently decreased locomotor activity and obviously enhanced sleep in rats (3-30 mg/kg) and dogs (0.25 and 0.5 mg/kg)[1]. |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
Solubility Information | DMSO : 100 mg/mL (237.82 mM), Sonication is recommended.
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Keywords | Inhibitor | inhibit | MK6096 | MK 6096 | Orexin Receptor (OX Receptor) | Filorexant | Hypocretin Receptor | HCRT Receptor |
Inhibitors Related | L-368,899 hydrochloride | YNT-185 | Orexin 2 Receptor Agonist | IPSU | MK-3697 | DORA-22 | Orexin B, rat, mouse Acetate | OXA (17-33) acetate | PF3274167 | ACT-462206 | Seltorexant | TCS 1102 |
Related Compound Libraries | Pain-Related Compound Library | Anti-Neurodegenerative Disease Compound Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Bioactive Compounds Library Max | GPCR Compound Library | Anti-Cancer Drug Library |