| CAS | 168482-23-3 |
| Sequence | Ac-Nle-cyclo(-Asp-His-D-2-Nal-Arg-Trp-Lys-NH2) |
| Sequence Single | Ac-Nle-cyclo(-DH-D-2-Nal-RWK-NH2) |
| Molecular Formula | C54H71N15O9 |
| Molecular Weight | 1074.25 |
| Synonyms | SHU9119 |
| Technology | Synthetic |
| Storage | -20°C, avoid light, cool and dry place |
| Application | Obesity Research|Pituitary & Hypothalamic Hormones |
| Description | Acetyl-(Nle4,Asp5,D-2-Nal7,Lys10)-cyclo-α-MSH (4-10) amide also called SHU9119, is a potent human melanocortin 3 and 4 receptors (MC3/4R) antagonist and a partial MC5R agonist; with IC50 values of 0.23, 0.06, and 0.09 nM for human MC3R, MC4R and MC5R, respectively. |
| References | 1. Characterization of a 41-residue ovine hypothalamic peptide that stimulates secretion of corticotropin and beta-endorphin. W.Vale et al., Science, 213, 1394 (1981) 2. 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. V.J.Hruby et al., J. Med. Chem., 38, 3454 (1995) 3. Further structure-activity studies of lactam derivatives of MT-II and SHU-9119: their activity and selectivity at human melanocortin receptors 3, 4, and 5. Grieco P, et al. Peptides. 2007 Jun;28(6):1191-6. 4. The central melanocortin system directly controls peripheral lipid metabolism. Nogueiras R, et al. J Clin Invest. 2007 Nov;117(11):3475-88. 5. Inhibition of the central melanocortin system decreases brown adipose tissue activity. Kooijman S, et al. J Lipid Res. 2014 Oct;55(10):2022-32. |
Acetyl-(Nle4,Asp5,D-2-Nal7,Lys10)-cyclo-α-MSH (4-10) amide
CAS No.: 168482-23-3
Acetyl-(Nle4,Asp5,D-2-Nal7,Lys10)-cyclo-α-MSH (4-10) amide also called SHU9119, is a potent human melanocortin 3 and 4
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