Cat. No. Name Size Price Add Cart
KI2026MK-43055 mg$154
MK-430510 mg$272
MK-430550 mg$912
MK-4305200 mg$2920

Chemical Characteristic

Product NameMK-4305
SynonymsSuvorexant
CAS No.1030377-33-3
Molecular Weight 450.92
FormulaC23H23ClN6O2
Chemical Name5-Chloro-2-[(5R)-5-methyl-4-[5-methyl-2-(2H-1,2,3-triazol-2-yl)benzoyl]-1,4-diazepan-1-yl]-1,3-benzoxazole
Smileso1c(nc2c1ccc(c2)Cl)N1CCN([C@@H](CC1)C)C(=O)c1c(ccc(c1)C)n1nccn1
Chemical Structure

Biological activities

MK-4305 is a potent and selective dual antagonist of OX1R and OX2R with Ki values of 0.55 and 0.35 nM, respectively. In telemetry-implanted rats, MK-4305 treatment (30 mg/kg) significantly increases rapid-eye movement (REM) and decreases delta sleep in active wake.[1] Orally administration of MK-4305 also significantly and dose-dependently reduces locomotor activity and promotes sleep in rats (10, 30, and 100 mg/kg), dogs (1 and 3 mg/kg), and rhesus monkeys (10 mg/kg) in vivo.[2]

References

[1] Cox CD, et al. Discovery of the dual orexin receptor antagonist [(7R)-4-(5-chloro-1,3-benzoxazol-2-yl)-7-methyl-1,4-diazepan-1-yl][5-methyl-2-(2H-1,2,3-triazol-2-yl)phenyl]methanone (MK-4305) for the treatment of insomnia. J Med Chem. 2010, 53(14): 5320-5332.
[2] Winrow CJ, et al. Promotion of sleep by suvorexant-a novel dual orexin receptor antagonist. J Neurogenet. 2011, 25(1-2): 52-61.

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