1044586-68-6
Chemical Structure
MK-5596
- CAS No.: 1044586-68-6
- Formula:C27H23Cl3N4O2
- Molecular Weight:541.86
IUPAC Name: (R)-N-(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
InChIKey: IDUFEEHNNASCMH-HSZRJFAPSA-N
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
Biological Activity: 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].
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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. | |||||||||||||||||||||
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References
- [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. [Content Brief]
