SHU 9119

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SHU 9119
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Description: MC3 and MC4 antagonist; MC5 partial agonist

Purity: ≥95%

Product Details
Citations (7)
Supplemental Products

Biological Activity

SHU 9119 is a 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


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

Soluble to 0.20 mg/ml in water
Store at -20°C

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.

Background References

  1. MC4R-dependent suppression of appetite by bone-derived lipocalin 2
    I Mosialou, S Shikhel, JM Liu, A Maurizi, N Luo, Z He, Y Huang, H Zong, RA Friedman, J Barasch, P Lanzano, L Deng, RL Leibel, M Rubin, T Nicholas, W Chung, LM Zeltser, KW Williams, JE Pessin, S Kousteni
    Nature, 2017;543(7645):385-390.
  2. Cardiovascular responses to chemical stimulation of the hypothalamic arcuate nucleus in the rat: role of the hypothalamic paraventricular nucleus.
    Kawabe, Tetsuya, Kawabe, Kazumi, Sapru, Hreday N
    PLoS ONE, 2012;7(9):e45180.
  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
  4. The central melanocortin system directly controls peripheral lipid metabolism.
    Nogueiras et al.
    J.Clin.Invest., 2007;117:3475
  5. 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

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