Biological Activity
Potent and selective melanocortin 4 (MC4) receptor agonist (IC50 values are 0.58 and 55 nM for human MC4 and MC3 receptors respectively). Produces a rapid and dose dependent restoration of cardiovascular and respiratory function in hemorrhage-shocked rats.
Technical Data
| M. Wt | 1180.41 |
| Formula | C59H85N15O11 |
| Sequence |
XDPFRWKPV (Modifications: X-1 = Ac-Nle, Phe-4 = D-Phe, Val-9 = C-terminal amide, Asp-2, Lys-7, Cyclized) |
| Storage | Store at -20°C |
| CAS Number | 667430-81-1 |
| PubChem ID | 90489007 |
| InChI Key | WOFDJLFPEWSAPJ-RVBGBMFGSA-N |
| Smiles | CCCCC(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=CC=CC=C2)NC(=O)[C@@H]2CCCN2C1=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](C(C)C)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 2 mg/ml in 25% ethanol / water |
Preparing Stock Solutions
The following data is based on the product molecular weight 1180.41. 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 | 0.85 mL | 4.24 mL | 8.47 mL |
| 5 mM | 0.17 mL | 0.85 mL | 1.69 mL |
| 10 mM | 0.08 mL | 0.42 mL | 0.85 mL |
| 50 mM | 0.02 mL | 0.08 mL | 0.17 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Giuliani et al (2007) Selective melanocortin MC4 receptor agonists reverse haemorrhagic shock and prevent multiple organ damage. Br.J.Pharmacol. 150 595 PMID: 17245369
Grieco et al (2003) Extensive structure-activity studies of lactam derivatives of MT-II and SHU-9119: their activity and selectivity at human melanocortin receptors 3, 4, and 5. J.Pept.Res. 62 199 PMID: 14531843
Keywords: PG 931, supplier, PG931, Potent, selective, MC4R, receptors, agonists, Melanocortin, Melanocortin, Receptors, Melanocortin, Receptors, Tocris Bioscience
