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.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
Phase 1
Isoform
OX1 Receptor; OX2 Receptor
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