For research use only. Not for therapeutic Use.
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].
MK-1064 (30 mg/kg, oral administration) promotes sleep in rodents selectively through OX2R in Wild-type mice[2].
MK-1064 (30 mg/kg, oral administration, 5 days) reverses the struggle behavior induced by CNO pre-treatment in rats[3].
MK-1064 (1-5 mg/kg, intravenous injection/oral administration) shows moderate oral bioavailability and clearance in rat, dog, and rhesus monkey[1].
| Catalog Number | I000771 |
| CAS Number | 1207253-08-4 |
| Synonyms | 5-(5-chloropyridin-3-yl)-N-[(5,6-dimethoxypyridin-2-yl)methyl]-2-pyridin-2-ylpyridine-3-carboxamide |
| Molecular Formula | C24H20ClN5O3 |
| Purity | ≥95% |
| InChI | InChI=1S/C24H20ClN5O3/c1-32-21-7-6-18(30-24(21)33-2)14-29-23(31)19-10-16(15-9-17(25)13-26-11-15)12-28-22(19)20-5-3-4-8-27-20/h3-13H,14H2,1-2H3,(H,29,31) |
| InChIKey | CKTWQGHVNRYNCM-UHFFFAOYSA-N |
| SMILES | COC1=C(N=C(C=C1)CNC(=O)C2=C(N=CC(=C2)C3=CC(=CN=C3)Cl)C4=CC=CC=N4)OC |
| Reference | [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. |
