Suvorexant (MK-4305)

Catalog No.S7279

Suvorexant (MK-4305) Chemical Structure

Molecular Weight(MW): 450.92

Suvorexant (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. Phase 3.

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

Biological Activity

Description Suvorexant (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. Phase 3.
Features Dual OX antagonist currently in Phase III clinical trials for the modulation of sleep.
Targets
OX2 receptor [1] OX1 receptor [1]
0.35 nM(Ki) 0.55 nM(Ki)
In vivo Suvorexant has excellent passive permeability and oral bioavailability, and induces favorable sleep effects in rats. [1] In addition, suvorexant 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). [2]

Protocol

Animal Research:[1]
+ Expand
  • Animal Models: Adult male Sprague−Dawley rats
  • Formulation: 20% aqueous solution of TPGS
  • Dosages: ~10 mg/kg
  • Administration: Oral gavage
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 10 mg/mL (22.17 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
In vivo 4% DMSO+10% PEG 400+10% Tween 80 5 mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 450.92
Formula

C23H23ClN6O2

CAS No. 1030377-33-3
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03034018 Not yet recruiting Insomnia Brigham and Womens Hospital March 2017 Phase 4
NCT02849548 Recruiting Posttraumatic Stress Disorder Howard University|Georgetown-Howard Universities Center for Clinical and Translational Science July 2016 Phase 4
NCT02750306 Recruiting Insomnia|Alzheimers Disease Merck Sharp & Dohme Corp. May 2016 Phase 3
NCT02704754 Recruiting Insomnia|Posttraumatic Stress Disorder Howard University|Merck Sharp & Dohme Corp. May 2016 Phase 4
NCT02785406 Recruiting Cocaine Use Disorder|Anxiety The University of Texas Health Science Center, Houston|Peter F. McManus Charitable Trust May 2016 Phase 2
NCT02593682 Recruiting Panic Disorder University of California, San Francisco May 2016 Early Phase 1

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OX Receptor Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID