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Synonyms: (Ac-cyclo-[Nle4Asp5,D-Nal(2)7,Lys10]α-MSH-(4-10)-NH2) | SHU 9119 | SHU-9119
Compound class: Peptide or derivative
Comment: SHU9119 is a melanocortin MC3/MC4 receptor antagonist and MC5 receptor agonist. This ligand entry was updated in August 2023, to more fully render its stereochemistry.
Ligand Activity Visualisation Charts
These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.✖
1. Adan RA, Szklarczyk AW, Oosterom J, Brakkee JH, Nijenhuis WA, Schaaper WM, Meloen RH, Gispen WH. (1999)
Characterization of melanocortin receptor ligands on cloned brain melanocortin receptors and on grooming behavior in the rat.
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2. Hruby VJ, Lu D, Sharma SD, Castrucci AL, Kesterson RA, al-Obeidi FA, Hadley ME, Cone RD. (1995)
Cyclic lactam alpha-melanotropin analogues of Ac-Nle4-cyclo[Asp5, D-Phe7,Lys10] alpha-melanocyte-stimulating hormone-(4-10)-NH2 with bulky aromatic amino acids at position 7 show high antagonist potency and selectivity at specific melanocortin receptors.
J Med Chem, 38 (18): 3454-61. [PMID:7658432]
3. MacNeil DJ, Howard AD, Guan X, Fong TM, Nargund RP, Bednarek MA, Goulet MT, Weinberg DH, Strack AM, Marsh DJ et al.. (2002)
The role of melanocortins in body weight regulation: opportunities for the treatment of obesity.
Eur J Pharmacol, 440 (2-3): 141-57. [PMID:12007532]
4. Schiöth HB, Muceniece R, Mutulis F, Bouifrouri AA, Mutule I, Wikberg JE. (1999)
Further pharmacological characterization of the selective melanocortin 4 receptor antagonist HS014: comparison with SHU9119.
Neuropeptides, 33 (3): 191-6. [PMID:10657491]