| Protocol | In Vitro | In vitro activity: Suvorexant (also known as MK-4305) is a potent dual OX receptor antagonist with Ki of 0.55 nM and 0.35 nM for OX1 receptor and OX2 receptor, respectively. Suvorexant is developed by Merck for the treatment of insomnia. It is currently undergoing Phase III trials. Suvorexant works by turning off wakefulness rather than by inducing sleep. As a dual orexin receptor (OXR) antagonist (DORA), suvorexant (MK-4305) has shown promise for the treatmen to finsomnias and sleep disorders. Kinase Assay: MK-4305 is a potent antagonist of OX1 receptor and OX2 receptor with Ki values of 0.55 nM and 0.35 nM, respectively Cell Assay: In vitro study showed that MK-4305 possessed a clean ancillary profile (>10000-fold selectivity for OX2R) as determined by an MDS Pharma off-target screen of 170 enzymes, receptors, and ion channels. |
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| In Vivo | In a mice in-vivo study, suvorexant (25mg/kg) was tested in mice during the inactive phase (lights on) when sleep is naturally more prevalent and when orexin levels are normally low. It was found that suvorexant substantially disturbed the sleep architecture by selectively increasing REM during the first 4h after dosing. At the doses tested, suvorexant significantly decreased wake only during the first hour and IPSU did not affect wake time. These data suggest that OX2R preferring antagonists may have areduced tendency for perturbing NREM/REM architecture in comparison with DORAs |
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| Animal model | Mice |
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These protocols are for reference only. InvivoChem does not
independently validate these methods.
Preparing Stock Solutions
| Solvent volume to be added |
Mass (the weight of a compound) |
| Mother liquor concentration |
1mg | 5mg | 10mg | 20mg |
| 1mM | 2.2177 mL | 11.0884 mL | 22.1769 mL | 44.3538 mL |
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| 5mM | 0.4435 mL | 2.2177 mL | 4.4354 mL | 8.8708 mL |
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| 10mM | 0.2218 mL | 1.1088 mL | 2.2177 mL | 4.4354 mL |
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| 20mM | 0.1109 mL | 0.5544 mL | 1.1088 mL | 2.2177 mL |
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Quality Control Documentation
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![Competition kinetics curves for [3H]-EMPA binding to OX2-expressing (HEK293) cell membranes in the presence of increasing concentrations of EMPA, TCS-OX2-29, suvorexant and almorexant. Br J Pharmacol. 2014 Jan;171(2):351-63.](https://invivochem.net/wp-content/uploads/2023/05/CgAGTF2hljOAcpbgAAF0clpwgeU334.jpg)
