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Details

Stereochemistry ACHIRAL
Molecular Formula C24H20ClN5O3
Molecular Weight 461.9
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of MK-1064

SMILES

COC1=CC=C(CNC(=O)C2=CC(=CN=C2C3=NC=CC=C3)C4=CN=CC(Cl)=C4)N=C1OC

InChI

InChIKey=CKTWQGHVNRYNCM-UHFFFAOYSA-N
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)

HIDE SMILES / InChI
MK-1064 is an orexin 2 receptor antagonist patented by pharmaceutical company Merck & Co for the treatment of insomnia. MK-1064decreases 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. MK-1064, even at the very high dose did not show signs of an enhanced predisposition to cataplexy in the food-elicited cataplexy test. MK-1064 has now completed two Phase I studies focused on pharmacokinetics, safety and sleep in healthy volunteers. The effects of MK-1064 on sleep parameters were moderate, but statistically significant, representing the first demonstration of PSG-quantified sleep induced in humans by an OX2R antagonist. MK-1064 at 50, 120 and 250 mg decreased latency to persistent sleep and wake after sleep onset, and increased total sleep time and sleep efficiency.

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
1789.0 nM [IC50]
18.0 nM [IC50]
PubMed

PubMed

TitleDatePubMed
Synthesis of [(11)C]MK-1064 as a new PET radioligand for imaging of orexin-2 receptor.
2016 Aug 1
Patents

Sample Use Guides

50, 120 and 250 mg
Route of Administration: Oral
Name Type Language
MK-1064
Common Name English
5''-CHLORO-N-((5,6-DIMETHOXYPYRIDIN-2-YL)METHYL)-2,2':5',3''-TERPYRIDINE-3'-CARBOXAMIDE
Systematic Name English
(2,2':5',3''-TERPYRIDINE)-3'-CARBOXAMIDE, 5''-CHLORO-N-((5,6-DIMETHOXY-2-PYRIDINYL)METHYL)-
Systematic Name English
MK 1064
Code English
5-(5-CHLORO-3-PYRIDYL)-N-((5,6-DIMETHOXY-2-PYRIDYL)METHYL)-2-(2-PYRIDYL)PYRIDINE-3-CARBOXAMIDE
Systematic Name English
Code System Code Type Description
SMS_ID
300000041499
Created by admin on Sat Dec 16 11:40:34 GMT 2023 , Edited by admin on Sat Dec 16 11:40:34 GMT 2023
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DRUG BANK
DB15028
Created by admin on Sat Dec 16 11:40:34 GMT 2023 , Edited by admin on Sat Dec 16 11:40:34 GMT 2023
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CAS
1207253-08-4
Created by admin on Sat Dec 16 11:40:34 GMT 2023 , Edited by admin on Sat Dec 16 11:40:34 GMT 2023
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FDA UNII
O812716S9E
Created by admin on Sat Dec 16 11:40:34 GMT 2023 , Edited by admin on Sat Dec 16 11:40:34 GMT 2023
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PUBCHEM
44633765
Created by admin on Sat Dec 16 11:40:34 GMT 2023 , Edited by admin on Sat Dec 16 11:40:34 GMT 2023
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