SHU 9119

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Cat.No. 3420 - SHU 9119 | Ac-Nle-cyclo(Asp-His-D-2-Nal-Arg-Trp-Lys)-NH2 | CAS No. 168482-23-3
Description: MC3 and MC4 antagonist; MC5 partial agonist
Datasheet
Citations (1)
Literature

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

M. Wt 1074.25
Formula C54H71N15O9
Sequence XDHXRWK

(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
CAS Number 168482-23-3
PubChem ID 9898183
InChI Key GGYWLZFXFKFWKL-XOJVSUSESA-N
Smiles CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@H](CC2=CNC3=C2C=CC=C3)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@@H](CC2=CC3=CC=CC=C3C=C2)NC(=O)[C@H](CC2=CNC=N2)NC1=O)C(N)=O

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.

Solubility Data

SolubilitySoluble to 0.20 mg/ml in water

Preparing Stock Solutions

The following data is based on the product molecular weight 1074.25. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 0.93 mL 4.65 mL 9.31 mL
5 mM 0.19 mL 0.93 mL 1.86 mL
10 mM 0.09 mL 0.47 mL 0.93 mL
50 mM 0.02 mL 0.09 mL 0.19 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

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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View Related Products by Target

Keywords: SHU 9119, supplier, MC3R, MC4R, antagonists, MC5R, partial, agonists, Receptors, Melanocortin, SHU9119, Melanocortin, Receptors, Tocris Bioscience

1 Citation 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


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