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MK-3697

MK-3697 is an isonicotinamide small molecule, acting as a potent and selective Orexin 2 receptor antagonist with Ki = 0.95 nM. IC50 value: 0.95 nM (Ki) Target: Orexin 2 receptor antagonist MK-3697 is a highly potent, orally bioavailable selective orexin 2 receptor antagonists (2-SORAs) that possess acceptable profiles for clinical development. Herein we report additional SAR studies within the “triaryl” amide 2-SORA series focused on improvements in compound stability in acidic media and time-dependent inhibition of CYP3A4. MK-3697 has improved stability and TDI profiles as well as excellent sleep efficacy across species.

Product Specifications

CAS Number

[1224846-01-8]

UNSPSC

12352005

Hazard Statement

H302-H315-H319-H335

Target

Orexin Receptor (OX Receptor)

Type

Reference compound

Related Pathways

GPCR/G Protein; Neuronal Signaling

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease; Endocrinology

Assay Protocol

https://www.medchemexpress.com/MK-3697.html

Purity

98.83

Solubility

DMSO : 22.5 mg/mL (ultrasonic; warming)

Smiles

O=C(C1=CC(C2=CC(C)=CN=C2)=NC=C1C3=NC=CS3)NCC4=NC(OC)=C(OC)C=C4

Molecular Formula

C23H21N5O3S

Molecular Weight

447.51

Precautions

P261-P264-P270-P271-P280-P302+P352-P304+P340-P305+P351+P338-P330-P362+P364-P403+P233-P405-P501

References & Citations

[1]Anthony J. Roecker, et al. Discovery of MK-3697: A Selective Orexin 2 Receptor Antagonist (2-SORA) for the Treatment of Insomnia. Bioorganic & Medicinal Chemistry Letters
 Available online 26 August 2014

Shipping Conditions

Room Temperature

Storage Conditions

-20°C, 3 years; 4°C, 2 years (Powder)

Scientific Category

Reference compound1

Clinical Information

Phase 2

Isoform

OX2 Receptor

Available Sizes

Curated Selection

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