Biological Activity
Highly potent melanocortin MC4 receptor antagonist (Ki values are 0.29, 18.6, 5.45 and 3.29 nM for cloned human MC4, MC1, MC3 and MC5 receptors respectively). Increases food intake, and blocks α-MSH- and MTII-induced hypotension and bradycardia in rats, following central administration in vivo.
Technical Data
| M. Wt | 1266.5 |
| Formula | C58H79N19O10S2 |
| Sequence |
CXRHXRWGC (Modifications: Cys-1 = N-terminal Ac, X-2 = Nle, X-5 = Nal, Cys-9 = C-terminal amide, Disulfide bridge between 1 - 9) |
| Storage | Desiccate at -20°C |
| CAS Number | 212370-59-7 |
| PubChem ID | 25081552 |
| InChI Key | PUOCNCOPVAOMDE-LQXMKOPKSA-N |
| Smiles | CCCC[C@@H]1NC(=O)[C@H](CSSC[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](CCCNC(N)=N)NC1=O)C(N)=O)NC(C)=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 0.50 mg/ml in water |
Preparing Stock Solutions
The following data is based on the product molecular weight 1266.5. 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 | 0.79 mL | 3.95 mL | 7.9 mL |
| 5 mM | 0.16 mL | 0.79 mL | 1.58 mL |
| 10 mM | 0.08 mL | 0.39 mL | 0.79 mL |
| 50 mM | 0.02 mL | 0.08 mL | 0.16 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Jonsson et al (2001) Melanocortin receptor agonist transiently increases oxygen consumption in rats. Neuroreport 12 3703 PMID: 11726778
Jonsson et al (2002) Food conversion is transiently affected during 4-week chronic administration of melanocortin agonist and antagonist in rats. J.Endocrinol. 173 517 PMID: 12065241
Kask et al (1998) Discovery of a novel superpotent and selective melanocortin-4 receptor antagonist (HS024): evaluation in vitro and in vivo. Endocrinology 139 5006 PMID: 9832440
Keywords: HS 024, supplier, potent, MC4R, receptor, antagonists, Receptors, Melanocortin, HS024, Melanocortin, Receptors, Melanocortin, Receptors, Tocris Bioscience
