Biological Activity
Potent melanocortin MC3 and MC4 receptor antagonist (IC50 values are 0.23 and 0.06 nM respectively) and MC5 partial agonist (EC50 = 0.12 nM). Upregulates expression of genes promoting lipogenesis and triglyceride storage (SCD1, LPL, ACCα and FAS), increases triglyceride synthesis and promotes insulin resistance. Increases food intake, body weight and fat mass when administered centrally in vivo.
Technical Data
| M. Wt | 1074.25 |
| Formula | C54H71N15O9 |
| Sequence |
XDHXRWK (Modifications: X-1 = Ac-Nle, X-4 = D-2-Nal, Lys-7 = C-terminal amide, cyclized Asp-2 - Lys-7) |
| Storage | Store at -20°C |
| CAS Number | 168482-23-3 |
| PubChem ID | 9898183 |
| InChI Key | GGYWLZFXFKFWKL-XOJVSUSESA-N |
| Smiles | CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@H](CC2=CNC3=C2C=CC=C3)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@@H](CC2=CC3=CC=CC=C3C=C2)NC(=O)[C@H](CC2=CNC=N2)NC1=O)C(N)=O |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solubility | Soluble to 0.20 mg/ml in water |
Preparing Stock Solutions
The following data is based on the product molecular weight 1074.25. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 0.93 mL | 4.65 mL | 9.31 mL |
| 5 mM | 0.19 mL | 0.93 mL | 1.86 mL |
| 10 mM | 0.09 mL | 0.47 mL | 0.93 mL |
| 50 mM | 0.02 mL | 0.09 mL | 0.19 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Hruby et al (1995) Cyclic lactam α-melanotropin analogues of Ac-Nle4-cyclo[Asp5,D-Phe7,Lys10] a-melanocyte-stimulating hormone-(4-10)-NH2 with bulky aromatic amino acids at position 7 show high antagonist potency a J.Med.Chem. 38 3454 PMID: 7658432
Grieco et al (2007) Further structure-activity studies with lactam derivatives of MT-II and SHU-9119: Their activity and selectivity at human melanocortin receptors 3, 4 and 5. Peptides 28 1191 PMID: 17482720
Nogueiras et al (2007) The central melanocortin system directly controls peripheral lipid metabolism. J.Clin.Invest. 117 3475 PMID: 17885689
Keywords: SHU 9119, supplier, MC3R, MC4R, antagonists, MC5R, partial, agonists, Receptors, Melanocortin, SHU9119, Melanocortin, Receptors, Melanocortin, Receptors, Tocris Bioscience
