Cat. No. 3420
Biological ActivityPotent 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)
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Certificate of Analysis / Product Datasheet / Safety Datasheet
References are publications that support the products' biological activity.
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.
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 and selectivity at specific melanocortin receptors. J.Med.Chem. 38 3454. PMID: 7658432.
If you know of a relevant reference for SHU 9119 please let us know.
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.
Do you know of a great paper that uses SHU 9119 from Tocris? If so please let us know.
View Related Products by Product Action
Keywords: SHU 9119, supplier, MC3R, MC4R, antagonists, MC5R, partial, agonists, Receptors, Melanocortin, SHU9119, Tocris Bioscience, Melanocortin (MC) Receptor products
Find multiple products by catalog number
New Products in this Area
Reverse analog of BradykininTASP 0390325
Potent and selective V1B receptor antagonist; orally bioavailableML 233
Non-peptide apelin receptor agonistBML 111
FPR2 (lipoxin A4 receptor) agonistAmylin (rat)
Potent endogenous peptide agonist for amylin, calcitonin, CGRP and adrenomedullin receptorsCalcitonin (human)
Endogenous calcitonin receptor agonist; inhibits bone resorption
Follow @Tocris on Twitter
Tocris is now actively tweeting. For regular updates on news, events and special offers, follow @Tocris on Twitter.