Setmelanotide (RM-493)

Catalog No.E1002 Batch:E100202

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)

In vivo (Add solvents to the product individually and in order)

Clear solution	5% DMSO 1 95% Corn oil	1.65mg/ml	Taking the 1 mL working solution as an example, add 50 μL 33 mg/ml clarified DMSO stock solution to 950 μL corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	5.0mg/ml	Taking the 1 mL working solution as an example, add 50 μL 100 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

* <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 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 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
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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