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Filorexant (MK-6096) is an orally bioavailable, effective, and selective reversible antagonist of OX1 and OX2 receptors, with (Ki <3 nM).

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $30 | In Stock | In Stock | |
| 5 mg | $68 | In Stock | In Stock | |
| 10 mg | $118 | In Stock | In Stock | |
| 25 mg | $198 | In Stock | In Stock | |
| 50 mg | $298 | In Stock | In Stock | |
| 100 mg | $437 | In Stock | In Stock | |
| 1 mL x 10 mM (in DMSO) | $76 | In Stock | In Stock |
| Description | Filorexant (MK-6096) is an orally bioavailable, effective, and selective reversible antagonist of OX1 and OX2 receptors, with (Ki <3 nM). |
| Targets&IC50 | OX receptor:< 3 nM(Ki) |
| 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]. |
| Synonyms | MK-6096 |
| Molecular Weight | 420.48 |
| Formula | C24H25FN4O2 |
| Cas No. | 1088991-73-4 |
| Smiles | C[C@@H]1CC[C@@H](COc2ccc(F)cn2)CN1C(=O)c1cc(C)ccc1-c1ncccn1 |
| Relative Density. | 1.203 g/cm3 (Predicted) |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 100 mg/mL (237.82 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 4 mg/mL (9.51 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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