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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- No. CAS: 1044586-68-6
- Fòrmula: C27H23Cl3N4O2
- Peso molecular:541.86
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
- Pureza y Documentación
- Referencias
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Help & FAQs
Actividad biológica
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CB1 1.0 nM (IC50) |
CYP3A4 3.3 μM (IC50) |
CB1 5.8 nM (EC50) |
CYP2C8 11 μM (IC50) |
CYP2C9 18 μM (IC50) |
CYP2D6 6 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | EC50 |
5.8 nM
Compound: 12C
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Inverse agonist activity at human recombinant cannabinoid CB1 receptor expressed in CHO cellssassessed as inhibition of forskolin-stimulated increase in intracellular cAMP level
Inverse agonist activity at human recombinant cannabinoid CB1 receptor expressed in CHO cellssassessed as inhibition of forskolin-stimulated increase in intracellular cAMP level
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[PMID: 20423086] |
| CHO | IC50 |
1 nM
Compound: 12C
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Displacement of [3H]CP-55940 from human recombinant cannabinoid CB1 receptor expressed in CHO cells
Displacement of [3H]CP-55940 from human recombinant cannabinoid CB1 receptor expressed in CHO cells
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[PMID: 20423086] |
| CHO | IC50 |
1500 nM
Compound: 12C
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Displacement of [3H]CP-55940 from human recombinant cannabinoid CB2 receptor expressed in CHO cells
Displacement of [3H]CP-55940 from human recombinant cannabinoid CB2 receptor expressed in CHO cells
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[PMID: 20423086] |
| HEK293 | IC50 |
1 μM
Compound: 12C
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Displacement of [35S]MK499 from human ERG expressed in HEK293 cells
Displacement of [35S]MK499 from human ERG expressed in HEK293 cells
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[PMID: 20423086] |
Chemical Information
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No. CAS 1044586-68-6
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Peso molecular 541.86
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Fòrmula C27H23Cl3N4O2
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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
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
[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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
MK-5596 Related Classifications
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