MK-1064
A potent, selective, orally bioavailable Orexin 2 receptor (OX2R) antagonist with Ki/IC50 of 0.5/18 nM; displays >100-fold selectivity over OX1R; promotes sleep and increases both rapid eye movement (REM) and non-REM (NREM) sleep in rats and dogs without inducing cataplexy; also decreases ACTH levels in rats.Sleep Disorder Preclinical (In Vitro) :MK-1064 (30 mg/kg, oral administration) promotes sleep in rodents selectively through OX2R in Wild-type mice.MK-1064 (30 mg/kg, oral administration, 5 days) reverses the struggle behavior induced by CNO pre-treatment in rats.MK-1064 (1-5 mg/kg, intravenous injection/oral administration) shows moderate oral bioavailability and clearance in rat, dog, and rhesus monkey.
Product Specifications
CAS Number
1207253-08-4
Product Name Alternative
MK1064 | MK 1064
Purity
>98% (HPLC)
Solubility
10 mM in DMSO
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
461.9003
Storage Conditions
Storage temperature: -20°C. Stability: ≥ 2 years
Notes
For research use only.
Other Product Names
[2,2':5',3''-Terpyridine]-3'-carboxamide, 5''-chloro-N-[ (5,6-dimethoxy-2-pyridinyl) methyl]-
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