Biological ActivitySHU 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.
(Modifications: X-1 = Ac-Nle, X-4 = D-2-Nal, Lys-7 = C-terminal amide, cyclized Asp-2 - Lys-7)
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For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
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.
The central melanocortin system directly controls peripheral lipid metabolism.
Nogueiras et al.
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.
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