MK-1064

• 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].

• 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

• CAS Number :

  [1207253-08-4]