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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.
| Molecular Weight | 420.48 |
| Formula | C24H25FN4O2 |
| CAS Number | 1088991-73-4 |
| Solubility (25°C) | DMSO 10 mM |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related OX Receptor Products |
|---|
| CVN766
CVN766 is an orally active inhibitor of orexin 1 receptor antagonist with blood-brain permeability with the IC50 values of 8 nM and >10 μM for OX1R and OX2R, respectively. |
| Nivasorexant
Nivasorexant is a potent orexin receptor antagonist. |
| [Ala11, D-Leu15]-Orexin B(human)
[Ala11,D-Leu15]-Orexin B(human) is a potent and selective orexin-2 receptor (OX2) agonist. |
| Orexin B, rat, mouse
Orexin B, rat, mouse (Rat orexin B) is an endogenous agonist at Orexin receptor with Kis of 420 and 36 nM for OX1 and OX2, respectively. |
| Hypocretin (70-98), human
Hypocretin (70-98), human is a polypeptide that is capable of binding to an orexin receptor OX1R and promotes apoptosis. |
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