Potent melanocortin MC3
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
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All Tocris products are intended for laboratory research use only.
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.
The central melanocortin system directly controls peripheral lipid metabolism.
Nogueiras et al.
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 citations listed below are publications that use Tocris products. Selected citations for SHU 9119 include:
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