Basic information Safety Supplier Related

mk-1064

Basic information Safety Supplier Related

mk-1064 Basic information

Product Name:
mk-1064
Synonyms:
  • mk-1064
  • 5''-Chloro-N-[(5,6-dimethoxypyridin-2-yl)methyl]-2,2':5',3''-terpyridine-3'-carboxamide
  • MK-1064(Urokinase inhibitor 1)
  • 5-(5-CHLOROPYRIDIN-3-YL)-N-[(5,6-DIMETHOXYPYRIDIN-2-YL)METHYL]-2-PYRIDIN-2-YLPYRIDINE-3-CARBOXAMIDE
  • MK-1064, CID 44633765
  • CS-2221
  • MK1064;MK 1064
  • [2,2':5',3''-Terpyridine]-3'-carboxamide, 5''-chloro-N-[(5,6-dimethoxy-2-pyridinyl)methyl]-
CAS:
1207253-08-4
MF:
C24H20ClN5O3
MW:
461.9
Mol File:
1207253-08-4.mol
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mk-1064 Chemical Properties

Boiling point:
662.4±55.0 °C(Predicted)
Density 
1.305±0.06 g/cm3(Predicted)
storage temp. 
Store at -20°C
solubility 
DMSO:60.0(Max Conc. mg/mL);129.9(Max Conc. mM)
form 
A crystalline solid
pka
11.98±0.46(Predicted)
color 
White to off-white
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Safety Information

HS Code 
2933399990
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mk-1064 Usage And Synthesis

Uses

MK-1064 is a selective and orally active OX2R antagonist (Ki: 0.5 nM, IC50: 18 nM). MK-1064 promotes sleep in vivo. MK-1064 can be used in the research of insomnia[1][3].

in vivo

MK-1064 (30?mg/kg, oral administration) promotes sleep in rodents selectively through OX2R in Wild-type mice[2].
MK-1064 (30?mg/kg, oral administration, 5 days) reverses the struggle behavior induced by CNO pre-treatment in rats[3].
MK-1064 (1-5 mg/kg, intravenous injection/oral administration) shows moderate oral bioavailability and clearance in rat, dog, and rhesus monkey[1].

Animal Model:Wild-type and OX2R knockout mice[2]
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)[1]
Dosage:1, 2, 3, 5 mg/kg
Administration:Oral administration (P.O.), intravenous injection (I.V.)
Result:Pharmacokinetics profile of MK-1064.
SpeciesDose (mg/kg) CL (mL/min/kg) t1/2 (h) Dose (mg/kg)Cmax (μM) F (%)
Rat2 (I.V.)390.35 (P.O.)1.554
Dog1 (I.V.)161.03 (P.O.)1.048
Rhesus2 (I.V.)120.85 (P.O.)0.916

IC 50

OX2 Receptor: 18 nM (IC50); OX1 Receptor: 1789 nM (IC50); OX2 Receptor: 0.5 nM (Ki); OX1 Receptor: 1584 nM (Ki)

References

[1] Roecker AJ et al. Discovery of 5''-chloro-N-[(5,6-dimethoxypyridin-2-yl)methyl]-2,2':5',3''-terpyridine-3'-carboxamide (MK-1064): a selective orexin 2 receptor antagonist (2-SORA) for the treatment of insomnia. ChemMedChem. 2014 Feb;9(2):311-22. DOI:10.1002/cmdc.201300447
[2] Gotter AL et al. Orexin 2 Receptor Antagonism is Sufficient to Promote NREM and REM Sleep from Mouse to Man. Sci Rep. 2016 Jun 3;6:27147. DOI:10.1038/srep27147
[3] Laura A Grafe, et al. Orexin 2 receptor regulation of the hypothalamic-pituitary-adrenal (HPA) response to acute and repeated stress. Neuroscience. 2017 Apr 21;348:313-323. DOI:10.1016/j.neuroscience.2017.02.038

mk-1064Supplier

WUHAN SUN-SHINE BIO-TECHNOLOGY Co., Ltd.
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17702719238 18971495150;
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sales@sun-shinechem.com
MedChemexpress LLC
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021-58955995
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Shanghai Lollane Biological Technology Co.,Ltd.
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Shanghai EFE Biological Technology Co., Ltd.
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021-65675885 18964387627
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Shanghai YuanYe Biotechnology Co., Ltd.
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021-61312847; 18021002903
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3008007409@qq.com
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