Free shipping on all orders over $ 500

MK-6096

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

Quality Control
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%
Solubility
Storage at -20°C
References

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.

Related OX Receptor Products
SB-334867

SB-334867 is a selective non-peptide orexin OX1 receptor antagonist with a pKb value of 7.2.

TCS-1102

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

MK-3697 is an isonicotinamide small molecule, acting as a potent and selective Orexin 2 receptor antagonist with Ki = 0.95 nM.

SB408124

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.

Suvorexant

Suvorexant (MK-4305) is a potent, selective and orally bioavailable antagonist of OX(1)R and OX(2)R for the treatment of insomnia.

  Catalog
Abmole Inhibitor Catalog 2017




Keywords: MK-6096 supplier, OX Receptor, inhibitors

Contact Us

Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2017 AbMole BioScience. All Rights Reserved.