MK-1064

Research use only, not for human use.

A potent, selective, orally bioavailable Orexin 2 receptor (OX2R) antagonist with Ki/IC50 of 0.5/18 nM.

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.

——

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. Animal Model:Wild-type and OX2R knockout miceDosage:30 mg/kg Administration:Oral administration Result:Displayed active wake reduction accompanied by significant increases in SWS (slow-wave sleep) and REM (rapid eye movement) at time points up to 3.5?hours following treatment. Animal Model:Rat, dog, and rhesus monkey (Pharmacokinetics assay)Dosage:1, 2, 3, 5 mg/kg Administration:Oral administration (P.O.), intravenous injection (I.V.)Result:Pharmacokinetics profile of MK-1064.

MK1064 | MK 1064

GPCR/G Protein

Orexin Receptor

OX2

Neurological Disease

Sleep Disorder

1207253-08-4

461.9003

C24H20ClN5O3

>98% (HPLC)

10 mM in DMSO

O=C(C1=CC(C2=CC(Cl)=CN=C2)=CN=C1C3=NC=CC=C3)NCC4=NC(OC)=C(OC)C=C4

[2,2':5',3''-Terpyridine]-3'-carboxamide, 5''-chloro-N-[(5,6-dimethoxy-2-pyridinyl)methyl]-

(-20℃)

With Ice Pack

≥ 2 years