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.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|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.
|Solubility||DMSO 10 mM|
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.
|Related OX Receptor Products|
SB-649868 is a selective orally active orexin (OX) receptor antagonist with pKi values of 9.4 and 9.5 at the OX1 and OX2 receptor, respectively.
SB-334867 is a selective non-peptide orexin OX1 receptor antagonist with a pKb value of 7.2.
TCS 1102 is a potent, dual orexin receptor antagonist (Ki values are 0.2 and 3 nM for OX2 and OX1 receptors respectively).
MK-3697 is an isonicotinamide small molecule, acting as a potent and selective Orexin 2 receptor antagonist with Ki = 0.95 nM.
SB408124 (Tocris-1963) is a non-peptide antagonist for OX1 receptor with Ki of 57 nM and27 nM in both whole cell and membrane, respectively, exhibits 50-fold selectivity over OX2 receptor.
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