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Cat. No. M2124
MK-6096 Structure
Size Price Availability Quantity
10mg USD 250 In stock
50mg USD 650 In stock
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Biological Activity

MK-6096 is an orally bioavailable potent and selective reversible antagonist of Orexin 1 Receptor (OX(1)R) and Orexin 2 Receptor (OX(2)R). In radioligand binding and functional cell based assays MK-6096 demonstrated potent binding and antagonism of both human OX(1)R and OX(2)R (<3 nM in binding, 11 nM in FLIPR), with no significant off-target activities against a panel of >170 receptors and enzymes. MK-6096 occupies 90% of human OX(2)Rs expressed in transgenic rats at a plasma concentration of 142 nM, and dose-dependently reduced locomotor activity and significantly increased sleep in rats (3-30 mg/kg) and dogs (0.25 and 0.5 mg/kg). MK-6096 represents a novel and selective therapeutic for the treatment of insomnia. MK-6096 has exceptional in vivo activity in preclinical sleep models.

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 420.48
Formula C24H25FN4O2
CAS Number 1088991-73-4
Purity >99%
Storage at -20°C

Discovery of [(2R,5R)-5-{[(5-fluoropyridin-2-yl)oxy]methyl}-2-methylpiperidin-1-yl][5-methyl-2-(pyrimidin-2-yl)phenyl]methanone (MK-6096): a dual orexin receptor antagonist with potent sleep-promoting properties.
Coleman PJ, et al. ChemMedChem. 2012 Mar 5;7(3):415-24, 337. PMID: 22307992.

Pharmacological characterization of MK-6096 - a dual orexin receptor antagonist for insomnia.
Winrow CJ, et al. Neuropharmacology. 2012 Feb;62(2):978-87. PMID: 22019562.

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Abmole Inhibitor Catalog 2017

Keywords: MK-6096 supplier, OX Receptor, inhibitors

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