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Submit ReviewBMS 470539 dihydrochloride
Description: Potent, selective MC1 receptor agonist
Chemical Name: 1-[1-(3-Methyl-L-histidyl-O-methyl-D-tyrosyl)-4-phenyl-4-piperidinyl]-1-butanone dihydrochloride
Purity: ≥98% (HPLC)
Biological Activity for BMS 470539 dihydrochloride
BMS 470539 dihydrochloride is a potent, selective melanocortin MC1 receptor agonist (IC50 = 120 nM). Exhibits anti-inflammatory properties following ischemia-reperfusion in the vasculature. Inhibits leukocyte trafficking.
Technical Data for BMS 470539 dihydrochloride
| M. Wt | 632.62 |
| Formula | C32H41N5O4.2HCl |
| Storage | Desiccate at RT |
| Purity | ≥98% (HPLC) |
| CAS Number | 2341796-82-3 |
| 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Product Datasheets for BMS 470539 dihydrochloride
References for BMS 470539 dihydrochloride
References are publications that support the biological activity of the product.
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
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Keywords: BMS 470539 dihydrochloride, BMS 470539 dihydrochloride supplier, BMS470539, melanocortin, agonist, MC1, agonists, anti-inflammatory, 457893-92-4, Melanocortin, Receptors, 4053, Tocris Bioscience
1 Citation for BMS 470539 dihydrochloride
Citations are publications that use Tocris products. Selected citations for BMS 470539 dihydrochloride include:
Jain et al (2018) Melanotan II causes hypothermia in mice by activation of mast cells and stimulation of histamine 1 receptors. Am J Physiol Endocrinol Metab 315 E357 PMID: 29812984
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Peptides Involved in Appetite Modulation Scientific Review
Written by Sonia Tucci, Lynsay Kobelis and Tim Kirkham, this review provides a synopsis of the increasing number of peptides that have been implicated in appetite regulation and energy homeostasis; putative roles of the major peptides are outlined and compounds available from Tocris are listed.