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Setmelanotide

Name: Setmelanotide
Brand: TargetMol
SKU: T12882
Price: 48 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T12882Cas No. 920014-72-8

Alias RM-493, RM493, IRC-022493, IRC022493, BIM-22493, BIM22493

Setmelanotide (RM-493) is a selective melanocortin-4 receptor agonist with EC50 values of 0.27 and 0.28 nM for human and rat MC4R. Setmelanotide enhances cAMP signaling, demonstrates functional selectivity, activates sympathetic preganglionic neurons to influence blood pressure, and is widely used to probe MC4R-MRAP2 interactions. Setmelanotide contributes to obesity-related research by modulating hunger and satiety circuits, reversing risperidone-induced weight gain in mice, and helping characterize MC4R variants in pediatric metabolic disorders. The anti-inflammatory actions of Setmelanotide in astrocytoma cells and the utility in combination with calorie restriction further highlight its broad value in metabolic and neuroendocrine research.

Setmelanotide

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Purity: 99.93%

Catalog No. T12882Alias RM-493, RM493, IRC-022493, IRC022493, BIM-22493, BIM22493Cas No. 920014-72-8

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$48	In Stock	In Stock
5 mg	$113	In Stock	In Stock
10 mg	$185	In Stock	In Stock
25 mg	$297	In Stock	In Stock
50 mg	$446	-	In Stock
100 mg	$645	-	In Stock
1 mL x 10 mM (in DMSO)	$218	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Purity:99.93%

Appearance:Solid

Color:White

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COA MS HPLC

Product Introduction

Bioactivity

Description	Setmelanotide (RM-493) is a selective melanocortin-4 receptor agonist with EC50 values of 0.27 and 0.28 nM for human and rat MC4R. Setmelanotide enhances cAMP signaling, demonstrates functional selectivity, activates sympathetic preganglionic neurons to influence blood pressure, and is widely used to probe MC4R-MRAP2 interactions. Setmelanotide contributes to obesity-related research by modulating hunger and satiety circuits, reversing risperidone-induced weight gain in mice, and helping characterize MC4R variants in pediatric metabolic disorders. The anti-inflammatory actions of Setmelanotide in astrocytoma cells and the utility in combination with calorie restriction further highlight its broad value in metabolic and neuroendocrine research.
Targets&IC50	MC1R (human):3.9 nM (ki), MC1R (human):5.8 nM (EC50), MC5R (human):1600 nM (EC50), MC4R (rat):0.28 Nm (EC50), MC3R (human):5.3nM (EC50), MC4R (human):0.27 nM (EC50), MC5R (human):430 nM (ki), MC4R (human):2.1 nM (ki), MC3R (human):10 nM (ki), MC4R (rat):2.7 nM (ki)
In vitro	Melanocortin receptor agonists act in the brain to regulate food intake and body weight, and also exert additional independent effects. Setmelanotide exhibits agonistic activity toward the melanocortin 4 receptor (MC4R) in both humans and rats, with a Ki value of 2.1 nM and an EC₅₀ value of 0.27 nM for human MC4R, and a Ki value of 2.7 nM and an EC₅₀ value of 0.28 nM for rat MC4R[1].
In vivo	The inhibitory effect of Setmelanotide on refeeding behavior in mice fasted overnight is receptor-specific, which is dependent on the mediation of functional MC4R but independent of MC3R. Compared with the control group, Lep⁰ᵇ/Lep⁰ᵇ mice treated with BIM-22493 exhibited significantly enhanced glucose clearance capacity. Moreover, chronic administration of BIM-22493 was associated with marked reductions in blood glucose levels and HOMA-IR index in mice[1]. In the diet-induced obese non-human primate model, an 8-week treatment with setmelanotide (13.5%) resulted in a transient 35% decrease in food intake and a concomitant sustained reduction in body weight[2].
Synonyms	RM-493, RM493, IRC-022493, IRC022493, BIM-22493, BIM22493

Chemical Properties

Molecular Weight	1117.31
Formula	C₄₉H₆₈N₁₈O₉S₂
Cas No.	920014-72-8
Smiles	C(C=1C=2C(NC1)=CC=CC2)[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](CC4=CC=CC=C4)NC(=O)[C@H](CC5=CN=CN5)NC(=O)[C@@H](C)NC(=O)[C@@H](NC([C@H](CCCNC(=N)N)NC(C)=O)=O)CSSC[C@@H](C(N)=O)NC3=O
Relative Density.	1.54 g/cm3 (Predicted)
Sequence	Ac-Arg-Cys(1)-D-Ala-His-D-Phe-Arg-Trp-Cys(1)-NH2
Sequence Short	RCAHFRWC

Storage & Solubility Information

Storage

keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

H2O: 50 mg/mL (44.75 mM), Sonication is recommended.

DMSO: 100 mg/mL (89.5 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween-80+45% Saline: 3.3 mg/mL (2.95 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

H2O/DMSO

	1mg	5mg	10mg	50mg
1 mM	0.8950 mL	4.4750 mL	8.9501 mL	44.7503 mL
5 mM	0.1790 mL	0.8950 mL	1.7900 mL	8.9501 mL
10 mM	0.0895 mL	0.4475 mL	0.8950 mL	4.4750 mL
20 mM	0.0448 mL	0.2238 mL	0.4475 mL	2.2375 mL

DMSO

	1mg	5mg	10mg	50mg
50 mM	0.0179 mL	0.0895 mL	0.1790 mL	0.8950 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc