Catalog Number: 3420
Biological Activity
Potent melanocortin MC3 and MC4 receptor antagonist (IC50 values are 0.23 and 0.06 nM respectively) and MC5 partial agonist (EC50 = 0.12 nM). Upregulates expression of genes promoting lipogenesis and triglyceride storage (SCD1, LPL, ACCα and FAS), increases triglyceride synthesis and promotes insulin resistance. Increases food intake, body weight and fat mass when administered centrally in vivo.
Technical Data
  • M.Wt:
    1074.25
  • Formula:
    C54H71N15O9
  • Sequence:
    XDHXRWK

    (Modifications: X-1 = Ac-Nle, X-4 = D-2-Nal, Lys-7 = C-terminal amide, cyclized Asp-2 - Lys-7)

  • Solubility:
    Soluble to 0.20 mg/ml in water
  • Storage:
    Store at -20°C
  • CAS No:
    168482-23-3
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. Cyclic lactam α-melanotropin analogues of Ac-Nle4-cyclo[Asp5,D-Phe7,Lys10] a-melanocyte-stimulating hormone-(4-10)-NH2 with bulky aromatic amino acids at position 7 show high antagonist potency a
    Hruby et al.
    J.Med.Chem., 1995;38:3454
  2. The central melanocortin system directly controls peripheral lipid metabolism.
    Nogueiras et al.
    J.Clin.Invest., 2007;117:3475
  3. Further structure-activity studies with lactam derivatives of MT-II and SHU-9119: Their activity and selectivity at human melanocortin receptors 3, 4 and 5.
    Grieco et al.
    Peptides, 2007;28:1191
Citations:

The citations listed below are publications that use Tocris products. Selected citations for SHU 9119 include:

1 Citations: Showing 1 - 1

  1. Ipsen 5i is a Novel Potent Pharmacoperone for Intracellularly Retained Melanocortin-4 Receptor Mutants.
    Authors: Tao and Huang
    Front Endocrinol (Lausanne) 2014;5:131

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