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MK-1064

Cat. No. M8997
MK-1064 Structure
Size Price Availability Quantity
5mg USD 210 In stock
10mg USD 330 In stock
25mg USD 660 In stock
50mg USD 960 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

MK-1064 is a potent, selective and orally active Orexin OX2 Receptor Antagonist for the research of insomnia. MK-1064 promotes sleep and increases both rapid eye movement (REM) and non-REM (NREM) sleep in rats at OX2R occupancies higher than the range observed for dual orexin receptor antagonists. Similar to dual antagonists, MK-1064 increases NREM and REM sleep in dogs without inducing cataplexy.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 461.9
Formula C24H20ClN5O3
CAS Number 1207253-08-4
Purity >98%
Solubility DMSO 10 mM
Storage at -20°C
References

Synthesis of [(11)C]MK-1064 as a new PET radioligand for imaging of orexin-2 receptor.
Gao M, et al. Bioorg Med Chem Lett. 2016 Aug 1;26(15):3694-9. PMID: 27268698.

Orexin 2 Receptor Antagonism is Sufficient to Promote NREM and REM Sleep from Mouse to Man.
Gotter AL, et al. Sci Rep. 2016 Jun 3;6:27147. PMID: 27256922.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: MK-1064 supplier, OX Receptor, inhibitors

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