Biological Activity
Potent, selective melanocortin MC1 receptor agonist (IC50 = 120 nM). Exhibits anti-inflammatory properties following ischemia-reperfusion in the vasculature. Inhibits leukocyte trafficking.
Compound Libraries
BMS 470539 dihydrochloride is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 632.62 |
| Formula | C32H41N5O4.2HCl |
| Storage | Desiccate at RT |
| Purity | ≥98% (HPLC) |
| CAS Number | 457893-92-4 |
| PubChem ID | 60210130 |
| InChI Key | DUAOBJHRUKFKIH-YDVFRNEYSA-N |
| Smiles | O=C(N2CCC(C(CCC)=O)(C4=CC=CC=C4)CC2)[C@H](NC([C@@H](N)CC3=CN=CN3C)=O)CC1=CC=C(OC)C=C1.Cl.Cl |
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
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 63.26 | 100 | |
| water | 63.26 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 632.62. 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 | 1.58 mL | 7.9 mL | 15.81 mL |
| 5 mM | 0.32 mL | 1.58 mL | 3.16 mL |
| 10 mM | 0.16 mL | 0.79 mL | 1.58 mL |
| 50 mM | 0.03 mL | 0.16 mL | 0.32 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Herpin et al (2003) Discovery of tyrosine-based potent and selective melanocortin-1 receptor small-molecule agonists with anti-inflammatory properties. J.Med.Chem. 46 1123 PMID: 12646021
Leoni et al (2010) The melanocortin MC1 receptor agonist BMS-470539 inhibits leukocyte trafficking in the inflamed vasculature. Br.J.Pharmacol. 160 171 PMID: 20331604
Kang (2006) A selective small molecule agonist of the melanocortin-1 receptor inhibits lipopolysaccharide-induced cytokine accumulation and leukocyte infiltration in mice. J.Leukoc.Biol. 80 897 PMID: 16888084
Keywords: BMS 470539 dihydrochloride, supplier, BMS470539, melanocortin, agonist, MC1, agonists, anti-inflammatory, Melanocortin, Receptors, Melanocortin, Receptors, Tocris Bioscience
