MK-1064

SKU: orb1226797

Description

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.

Key Properties

• CAS Number: 1207253-08-4
• MW: 461.9003
• Purity: >98% (HPLC)
• Formula: C₂₄H₂₀ClN₅O₃
• SMILES: O=C(C1=CC(C2=CC(Cl)=CN=C2)=CN=C1C3=NC=CC=C3)NCC4=NC(OC)=C(OC)C=C4
• Target: Orexin Receptor
• Solubility: 10 mM in DMSO

Bioactivity

• In Vivo:
  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 mice. Dosage: 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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

MK1064 | MK 1064

Quick Database Links

Gene Symbol

Orexin Receptor