MK-5596

MK-5596 is an efficient, selective and orally active CB1R (IC50 = 1.0 nM, EC50 = 5.8 nM) inverse agonist. MK-5596 has weak hERG inhibitory activity. MK-5596 has strong weight loss and appetite suppression effects. MK-5596 has a certain inhibitory effect on CYP enzymes (CYP3A4: IC50 = 3.3 μM, CYP2C8: IC50 = 11 μM, CYP2C9: IC50 = 18 μM, CYP2D6: IC50 = 6 μM) . MK-5596 can be used for research on conditions such as obesity[1].

Product Specifications

CAS Number

[1044586-68-6]

UNSPSC

12352005

Target

Cannabinoid Receptor; Cytochrome P450

Related Pathways

GPCR/G Protein; Metabolic Enzyme/Protease; Neuronal Signaling

Field of Research

Metabolic Disease

Smiles

ClC1=CC=C(C2=CC3=C(OC(C)(C)C[C@H]3NC(C4=NNC(C)=C4)=O)N=C2C5=C(Cl)C=C(Cl)C=C5)C=C1

Molecular Formula

C27H23Cl3N4O2

Molecular Weight

541.86

References & Citations

[1]Yan L, et al. Discovery of N-[ (4R) -6- (4-chlorophenyl) -7- (2,4-dichlorophenyl) -2,2-dimethyl-3,4-dihydro-2H-pyrano[2,3-b]pyridin-4-yl]-5-methyl-1H-pyrazole-3-carboxamide (MK-5596) as a novel cannabinoid-1 receptor (CB1R) inverse agonist for the treatment of obesity. J Med Chem. 2010 May 27;53 (10) :4028-37.