MK-1064

MK-1064 is a selective and orally active OX2R antagonist (Ki: 0.5 nM, IC50: 18 nM) . MK-1064 promotes sleep in vivo. MK-1064 can be used in the research of insomnia[1][3].

Product Specifications

CAS Number

[1207253-08-4]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Orexin Receptor (OX Receptor)

Type

Reference compound

Related Pathways

GPCR/G Protein; Neuronal Signaling

Applications

Cancer-programmed cell death

Field of Research

Cancer; Endocrinology

Assay Protocol

https://www.medchemexpress.com/MK-1064.html

Purity

99.95

Solubility

DMSO : 50 mg/mL (ultrasonic)

Smiles

O=C(C1=CC(C2=CC(Cl)=CN=C2)=CN=C1C3=NC=CC=C3)NCC4=NC(OC)=C(OC)C=C4

Molecular Formula

C24H20ClN5O3

Molecular Weight

461.90

Precautions

H302, H315, H319, H335

References & Citations

[1]Roecker AJ et al. Discovery of 5''-chloro-N-[ (5,6-dimethoxypyridin-2-yl) methyl]-2,2':5',3''-terpyridine-3'-carboxamide (MK-1064) : a selective orexin 2 receptor antagonist (2-SORA) for the treatment of insomnia. ChemMedChem. 2014 Feb;9 (2) :311-22. |[2]Gotter AL et al. Orexin 2 Receptor Antagonism is Sufficient to Promote NREM and REM Sleep from Mouse to Man. Sci Rep. 2016 Jun 3;6:27147. |[3]Laura A Grafe, et al. Orexin 2 receptor regulation of the hypothalamic-pituitary-adrenal (HPA) response to acute and repeated stress. Neuroscience. 2017 Apr 21;348:313-323.