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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
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
-
保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
生物活性
-
化学情報
- 純度とドキュメンテーション
- 参考文献
-
Help & FAQs
生物活性
|
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) |
|
Cell Line
|
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
-
CAS 番号 1044586-68-6
-
分子量 541.86
-
分子式 C27H23Cl3N4O2
-
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
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
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)
MK-5596 関連分類
HY-10575 関連分類
Powered by Bioz