MK-1064

MK-1064 is an orexin 2 receptor (OX2R) antagonist that is selective for OX2R over OX1R (IC50s = 18 and 1,789 nM, respectively). It decreases the amount of time spent in active wake and increases the time spent in rapid eye movement (REM) sleep and slow-wave sleep (SMS) in mice, rats, dogs, and rhesus monkeys when administered at doses of 100, 20, 1, and 10 mg/kg, respectively. MK-1064 (30 mg/kg) inhibits restraint stress-induced increases in plasma adrenocorticotropic hormone (ACTH) levels and struggle behavior, as well as decreases in body weight, in rats expressing the hM3Dq designer receptor exclusively activated by designer drugs (DREADD) activated by clozapine N-oxide (CNO, Cay-16882) in orexin neurons.Formal Name: 5''-chloro-N-[(5,6-dimethoxy-2-pyridinyl)methyl]-[2,2':5',3''-terpyridine]-3'-carboxamide. CAS Number: 1207253-08-4. Molecular Formula: C24H20ClN5O3. Formula Weight: 461.9. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, Ethanol: 2.5 mg/ml. lambdamax: 290 nm. SMILES: ClC1=CN=CC(C2=CN=C(C3=CC=CC=N3)C(C(NCC4=CC=C(OC)C(OC)=N4)=O)=C2)=C1. InChi Code: 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). InChi Key: CKTWQGHVNRYNCM-UHFFFAOYSA-N.