Catalog Number: 4053
Chemical Name: 1-[1-(3-Methyl-L-histidyl-O-methyl-D-tyrosyl)-4-phenyl-4-piperidinyl]-1-butanone dihydrochloride
Biological Activity
Potent, selective melanocortin MC1 receptor agonist (IC50 = 120 nM). Exhibits anti-inflammatory properties following ischemia-reperfusion in the vasculature. Inhibits leukocyte trafficking.
Technical Data
  • M.Wt:
    632.62
  • Formula:
    C32H41N5O4.2HCl
  • Solubility:
    Soluble to 100 mM in water and to 100 mM in DMSO
  • Purity:
    >98%
  • Storage:
    Desiccate at RT
  • CAS No:
    457893-92-4
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.
Background References
  1. A selective small molecule agonist of the melanocortin-1 receptor inhibits lipopolysaccharide-induced cytokine accumulation and leukocyte infiltration in mice.
    Kang
    J.Leukoc.Biol., 2006;80:897
  2. Discovery of tyrosine-based potent and selective melanocortin-1 receptor small-molecule agonists with anti-inflammatory properties.
    Herpin et al.
    J.Med.Chem., 2003;46:1123
  3. The melanocortin MC1 receptor agonist BMS-470539 inhibits leukocyte trafficking in the inflamed vasculature.
    Leoni et al.
    Br.J.Pharmacol., 2010;160:171

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