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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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 1044586-68-6
- 分子式: C27H23Cl3N4O2
- 分子量:541.86
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
製品説明
IC50 & Target
[1]|
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) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | EC50 |
5.8 nM
Compound: 12C
|
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
|
[PMID: 20423086] |
| CHO | IC50 |
1 nM
Compound: 12C
|
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
|
[PMID: 20423086] |
| CHO | IC50 |
1500 nM
Compound: 12C
|
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
|
[PMID: 20423086] |
| HEK293 | IC50 |
1 μM
Compound: 12C
|
Displacement of [35S]MK499 from human ERG expressed in HEK293 cells
Displacement of [35S]MK499 from human ERG expressed in HEK293 cells
|
[PMID: 20423086] |
化学情報
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CAS 番号 1044586-68-6
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分子量 541.86
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
プロトコル
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Research Protocol for Metabolic Diseases
AMP-activated protein kinase, AMPK, is a conserved cellular energy sensor that responds to reduced cellular energy status and coordinates metabolism by increasing ATP-generating catabolic pathways while suppressing ATP-consuming anabolic processes. In metabolic disease research, the AMPK pathway is experimentally relevant because it regulates hepatic lipid synthesis, fatty acid oxidation, glucose production, skeletal-muscle glucose disposal, mTORC1-linked biosynthesis, autophagy, mitochondrial homeostasis, and whole-body energy balance. The central pathway logic is that energy stress, metformin, exercise-like stimulation, or direct AMPK activators increase AMPKα Thr172 phosphorylation and downstream substrate phosphorylation, including ACC and RAPTOR. Phosphorylation of ACC suppresses lipogenesis and supports fatty acid oxidation, whereas phosphorylation of RAPTOR suppresses mTORC1 signaling and links cellular energy status to growth and protein synthesis control. The pathway is linked
純度とドキュメンテーション
参考文献
[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
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)