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Setmelanotide (RM-493)

Name: Setmelanotide (RM-493)
Brand: Selleck Chemicals
SKU: E1002

Synonyms: BIM-22493, CAM 4072

Catalog No.E1002 Purity: 99.76%

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.

Setmelanotide (RM-493) Chemical Structure

CAS: 920014-72-8

Purity & Quality Control

Batch: Purity: 99.76%

99.76

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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
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]
Cell Research	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.

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

References

Chemical lnformation & Solubility

Molecular Weight	1117.31	Formula	C₄₉H₆₈N₁₈O₉S₂
CAS No.	920014-72-8	SDF	--
Smiles	CC1NC(=O)C(CSSCC(NC(=O)C(CC2=C[NH]C3=CC=CC=C23)NC(=O)C(CCCN=C(N)N)NC(=O)C(CC4=CC=CC=C4)NC(=O)C(CC5=CN=C[NH]5)NC1=O)C(N)=O)NC(=O)C(CCCN=C(N)N)NC(C)=O
Storage (From the date of receipt)	3 years -20°C powder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years -20°C powder		1 month-20°Cin solvent

In vitro
Batch:

DMSO : 100 mg/mL ( (89.5 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 100 mg/mL

Ethanol : 100 mg/mL

Molecular Weight Calculator

In vivo
Batch:

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In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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