product name Suvorexant (MK-4305)
Description: 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.
References: J Med Chem. 2010 Jul 22;53(14):5320-32; Br J Pharmacol. 2014 Jan;171(2):351-63.
450.92
Formula
C23H23ClN6O2
CAS No.
1030377-33-3
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 10 mg/mL (22.2 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
4% DMSO+10% PEG 400+10% Tween 80: 5mg/mL
Synonyms
other peoduct :
| In Vitro |
In vitro activity: In vitro study showed that MK-4305 possesseed 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. 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 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 |
| Animal model | |
| Formulation & Dosage | |
| References | J Med Chem. 2010 Jul 22;53(14):5320-32; Br J Pharmacol. 2014 Jan;171(2):351-63. |
