Description: MC3 and MC4 antagonist; MC5 partial agonist
Biological Activity
Technical Data
Solubility
Calculators
Datasheets
References
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.
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
Solubility
Soluble 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.
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
Safety Datasheet
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References
References are publications that support the products' biological activity.
Hrubyet 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
Griecoet 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
Nogueiraset al (2007) The central melanocortin system directly controls peripheral lipid metabolism. J.Clin.Invest. 117 3475 PMID: 17885689