Biological Activity
Potent and selective melanocortin MC4 receptor antagonist (Ki values are 3.16, 108, 54.4 and 694 nM for cloned human MC4, MC1, MC3 and MC5 receptors respectively). Increases food intake in rats and nociception in mice following central administration in vivo. Also inhibits IL-1β-induced Fos expression in the paraventricular hypothalamus.
Technical Data
| M. Wt | 1563.77 |
| Formula | C71H94N20O17S2 |
| Sequence |
CEHXRWGCPPKD (Modifications: Cys-1 = N-terminal Ac, X = 2-Nal, Asp-12 = C-terminal amide, Disulfide bridge between 1 - 8) |
| Storage | Desiccate at -20°C |
| CAS Number | 207678-81-7 |
| PubChem ID | 24821295 |
| InChI Key | BRGDPINZISNYJL-VMAVSDBDSA-N |
| Smiles | CC(=O)N[C@H]1CSSC[C@H](NC(=O)CNC(=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)NC(=O)[C@H](CCC(O)=O)NC1=O)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCCN)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 1563.77. 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 | 0.64 mL | 3.2 mL | 6.39 mL |
| 5 mM | 0.13 mL | 0.64 mL | 1.28 mL |
| 10 mM | 0.06 mL | 0.32 mL | 0.64 mL |
| 50 mM | 0.01 mL | 0.06 mL | 0.13 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Bellasio et al (2003) Melanocortin receptor agonists and antagonists modulate nociceptive sensitivity in the mouse formalin test. Eur.J.Pharmacol. 482 127 PMID: 14660013
Schioth et al (1998) Discovery of novel melanocortin4 receptor selective MSH analogues. Br.J.Pharmacol. 124 75 PMID: 9630346
Whitaker and Reye (2008) Central blockade of melanocortin receptors attenuates the metabolic and locomotor responses to peripheral interleukin-1β administration. Neuropharmacology 54 509 PMID: 18082228
Keywords: HS 014, supplier, Selective, MC4R, receptor, antagonists, Receptors, Melanocortin, HS014, Melanocortin, Receptors, Melanocortin, Receptors, Tocris Bioscience
