Setmelanotide (RM-493)

Catalog No.E1002 Batch:E100201

Technical Data

Formula	C₄₉H₆₈N₁₈O₉S₂
Molecular Weight	1117.31	CAS No.	920014-72-8
Solubility (25°C)*	In vitro	DMSO	100 mg/mL (89.5 mM)
		Water	100 mg/mL (89.5 mM)
		Ethanol	100 mg/mL (89.5 mM)
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description

Setmelanotide (RM-493, BIM-22493, CAM 4072) is a cyclic peptide full agonist of melanocortin-4 receptor (MC4R) with an EC50 of 0.27 nM and a Ki of 2.1 nM.

Targets

MC4R ^[1]	MC4R ^[1]
0.27 nM(EC50)	2.1 nM(Ki)

In vitro

Setmelanotide decreases TNF-α/IFN-γ-induced chemokine expression in astrocytes and increases IL-6 and IL-11 mRNA and protein secretion via MC4R. Setmelanotide Induces CREB phosphorylation in astrocytes and setmelanotide treated astrocytes secrete factors that are able to modulate macrophage polarization into an anti-inflammatory phenotype.^[2]

In vivo

RM-493 and liraglutide co-treatment enhances weight loss in DIO mice and hypothalamic Glp-1r expression is higher in mice treated with the combination therapy after both acute and chronic treatment. Adjunctive administration of RM-493 and liraglutide improves glucose tolerance and insulin sensitivity, lowers fasting levels of glucose and insulin and decreases cholesterol levels beyond what can be achieved with the corresponding mono-therapies.^[3]

Protocol (from reference)

Cell Assay:^{^[2]}	Cell lines U373 astrocytoma cells Concentrations 0.001 μM –10 μM Incubation Time 1h, 4 h Method Cells were treated with 0.001–10 μM setmelanotide for 1 h and thereafter with TNF-α and IFN-γ for 4 h. For blocking experiments, 10 μM SHU9119 (26) was added 30 min before addition of setmelanotide during 4 h. Astrocytes stimulate with setmelanotide and or SHU9119 (10 μM) for 4 h, replace the medium with macrophage culture medium and add the medium to the macrophages 24 h thereafter. From the medium, 100 μL is collected in Eppendorf tubes and stored at −80°C for ELISA assays.
Animal Study:^{^[3]}	Animal Models Diet-induced obese mice Dosages 3.6 μmol/kg/day Administration s.c.

Cell Assay:^{^[2]}

Cell lines
U373 astrocytoma cells
Concentrations
0.001 μM –10 μM
Incubation Time
1h, 4 h
Method
Cells were treated with 0.001–10 μM setmelanotide for 1 h and thereafter with TNF-α and IFN-γ for 4 h. For blocking experiments, 10 μM SHU9119 (26) was added 30 min before addition of setmelanotide during 4 h. Astrocytes stimulate with setmelanotide and or SHU9119 (10 μM) for 4 h, replace the medium with macrophage culture medium and add the medium to the macrophages 24 h thereafter. From the medium, 100 μL is collected in Eppendorf tubes and stored at −80°C for ELISA assays.

Animal Study:^{^[3]}

Animal Models
Diet-induced obese mice
Dosages
3.6 μmol/kg/day
Administration
s.c.

References

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SHIPPING AND STORAGE
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