Biological Activity
Potent human MC1 receptor antagonist (IC50 = 17 nM). Also partial agonist at human MC3 and MC5 receptors (EC50 values are 59 and 1300 nM, respectively). Exhibits binding affinity for A375 melanoma cells in vitro. Reverses morphine-induced hyperalgesia in female mice, with no effect in male mice. γMSH analog.
Technical Data
| M. Wt | 1347.51 |
| Formula | C62H82N20O13S |
| Sequence |
XGHFRWCDRFG (Modifications: X = Butanoic acid, Gly-11 = C-terminal amide, Phe-4 = D-Phe, Trp-6 = D-Trp, carba sulfide bridge between X-1 - Cys-7) |
| Storage | Store at -20°C |
| CAS Number | 1416983-77-1 |
| PubChem ID | 122177131 |
| InChI Key | QJBNFEXQHBDMQM-VTWSTLNFSA-N |
| Smiles | NC(=O)CNC(=O)[C@H](CC1=CC=CC=C1)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CC(O)=O)NC(=O)[C@@H]1CSCCCC(=O)NCC(=O)N[C@@H](CC2=CNC=N2)C(=O)N[C@@H](CC2=CC=CC=C2)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC2=CNC3=C2C=CC=C3)C(=O)N1 |
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 1347.51. 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 | 0.74 mL | 3.71 mL | 7.42 mL |
| 5 mM | 0.15 mL | 0.74 mL | 1.48 mL |
| 10 mM | 0.07 mL | 0.37 mL | 0.74 mL |
| 50 mM | 0.01 mL | 0.07 mL | 0.15 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Cai et al (2013) An unusual conformation of γ-melanocyte-stimulating hormone analogues leads to a selective human melanocortin 1 receptor antagonist for targeting melanoma cells. Biochemistry 52 752 PMID: 23276279
Juni et al (2010) Sex-specific mediation of opioid-induced hyperalgesia by the melanocortin-1 receptor. Anesthesiology 112 181 PMID: 19996949
Arout et al (2015) Spinal and supraspinal N-methyl-D-aspartate and melanocortin-1 receptors contribute to a qualitative sex difference in morphine-induced hyperalgesia. Physiol.Behav. 147 364 PMID: 25982086
Keywords: MSG 606, supplier, MSG606, potent, MC1, receptors, melanocortin, antagonists, partial, agonists, MC3, MC5, hyperalgesia, Melanocortin, Receptors, Melanocortin, Receptors, Tocris Bioscience
