MK-1064

• UNSPSC Description:

  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].

• Target Antigen:

  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 Weight:

  461.90

• 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)

• Clinical Information:

  Phase 1

• CAS Number:

  1207253-08-4