Biological Activity
Potent and selective melanocortin MC4 receptor antagonist (IC50 values are 0.5 and 44.9 nM at MC4 and MC3 respectively) that antagonizes the effects of α-MSH. Suppresses thyrotropin-releasing hormone (TRH) release, attenuates food intake and reduces formalin-induced pain in vivo.
Technical Data
| M. Wt | 1506.72 |
| Formula | C69H91N19O16S2 |
| Sequence |
XEHXRWGCPPKD (Modifications: Disulfide bridge between 1 - 8, X-1 = Mpr, X-4 = D-2-Nal, Asp-12 = C-terminal amide) |
| Storage | Store at -20°C |
| CAS Number | 436083-30-6 |
| PubChem ID | 90488844 |
| InChI Key | DBHQKXPXPFYXHK-DUOXTXSESA-N |
| Smiles | NCCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC2=CNC=N2)C(=O)N[C@H](CC2=CC3=CC=CC=C3C=C2)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC2=CNC3=C2C=CC=C3)C(=O)NCC(=O)N1)C(=O)N[C@@H](CC(O)=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 1 mg/ml in water |
Preparing Stock Solutions
The following data is based on the product molecular weight 1506.72. 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 | 0.66 mL | 3.32 mL | 6.64 mL |
| 5 mM | 0.13 mL | 0.66 mL | 1.33 mL |
| 10 mM | 0.07 mL | 0.33 mL | 0.66 mL |
| 50 mM | 0.01 mL | 0.07 mL | 0.13 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Kim et al (2002) Effects of melanocortin receptor ligands on thyrotropin-releasing hormone release: evidence for the differential roles of melanocortin 3 and 4 receptors. J.Neuroendocrinol. 14 276 PMID: 11963824
Bellasio et al (2003) Melanocortin receptor agonists and antagonists modulate nociceptive sensitivity in the mouse formalin test. Eur.J.Pharmacol. 482 127 PMID: 14660013
Verty et al (2004) Evidence for an interaction between CB1 cannabinoid and melanocortin MCR-4 receptors in regulating food intake. Endocrinology 145 3224 PMID: 15033920
Keywords: JKC 363, supplier, Potent, selective, MC4R, receptor, antagonists, Receptors, Melanocortin, JKC363, Melanocortin, Receptors, Melanocortin, Receptors, Tocris Bioscience
