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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)
|Storage||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.
|Solubility||Soluble to 0.20 mg/ml in water|
References are publications that support the biological activity of the product.
Hruby et al (1995) 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 J.Med.Chem. 38 3454 PMID: 7658432
Grieco et al (2007) 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. Peptides 28 1191 PMID: 17482720
Nogueiras et al (2007) The central melanocortin system directly controls peripheral lipid metabolism. J.Clin.Invest. 117 3475 PMID: 17885689
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Keywords: SHU 9119, SHU 9119 supplier, MC3R, MC4R, antagonists, MC5R, partial, agonists, Receptors, Melanocortin, SHU9119, 3420, Tocris Bioscience
2 Citations for SHU 9119
Citations are publications that use Tocris products. Selected citations for SHU 9119 include:
Tao and Huang (2014) Ipsen 5i is a Novel Potent Pharmacoperone for Intracellularly Retained Melanocortin-4 Receptor Mutants. Front Endocrinol (Lausanne) 5 131 PMID: 25136332
Jeong et al (2018) Activation of temperature-sensitive TRPV1-like receptors in ARC POMC neurons reduces food intake. PLoS Biol 16 e2004399 PMID: 29689050
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