SHU 9119
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
(Modifications: X-1 = Ac-Nle, X-4 = D-2-Nal, Lys-7 = C-terminal amide, cyclized Asp-2 - Lys-7)
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
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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 -
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 -
The central melanocortin system directly controls peripheral lipid metabolism.
Nogueiras et al.
J.Clin.Invest., 2007;117:3475
Product Datasheets
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Citations for SHU 9119
The citations listed below are publications that use Tocris products. Selected citations for SHU 9119 include:
3 Citations: Showing 1 - 3
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A Neural Circuit for the Suppression of Pain by a Competing Need State.
Authors: Alhadeff Et al.
Cell 2018;173:140
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Activation of temperature-sensitive TRPV1-like receptors in ARC POMC neurons reduces food intake.
Authors: Jeong Et al.
PLoS Biol 2018;16:e2004399
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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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