Setmelanotide (RM-493)

Catalog No.E1002 Batch:E100202

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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)
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
5.0mg/ml
5% DMSO 95% Corn oil
1.65mg/ml
* <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.)

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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.

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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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