Art. -Nr.: HY-19870

Setmelanotide

(Synonyms: RM-493; BIM-22493; IRC-022493)

8 Cited Publications

Kundenbewertung

Based on 8 publication(s) in Google Scholar

Setmelanotide (RM-493) is a selective melanocortin 4 receptor (MC4R) agonist with EC₅₀s of 0.27 nM and 0.28 nM for human and rat MC4R, respectively.

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Reinheit: 99.99%
CAS. Nr.: 920014-72-8
Formel: C₄₉H₆₈N₁₈O₉S₂
Molecular Weight:1117.31

Speicherung:

Sealed storage, away from moisture.

Powder -80°C, 2 years , -20°C, 1 year

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Setmelanotide Chemical Structure

CAS. Nr.: 920014-72-8

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (8)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Setmelanotide (RM-493) is a selective melanocortin 4 receptor (MC4R) agonist with EC₅₀s of 0.27 nM and 0.28 nM for human and rat MC4R, respectively^[1].

IC₅₀ & Target

Ki:3.9 nM (hMC1R), 10 nM (hMC3R), 2.1 nM (hMC4R), 430 nM (hMC5R), 2.7 nM (rMC4R)^[1]
EC50: 5.8 nM (hMC1R), 5.3nM (hMC3R), 0.27 nM (hMC4R), 0.28 (rMC4R), 1600 nM (hMC5R)^[1]

Alle Melanocortin Receptor Isoform-spezifische Produkte anzeigen :

In Vitro

Melanocortin receptor agonists act in the brain to regulate food intake and body weight and, independently of these actions. Setmelanotide exhibits agonist activity to human and rat MC4R with K_is of 2.1 and 2.7 nM and EC₅₀s of 0.27 and 0.28 nM, respectively^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Inhibition of refeeding after an overnight fast by Setmelanotide is dependent on functional MC4R, and does not require MC3R. BIM-22493 acutely improves glucose homeostasis. Lep^ob/Lep^ob mice treated with BIM-22493 exhibits significantly improved glucose clearance when compared to controls. Chronic BIM-22493 treatment was associated with significantly lower levels of serum glucose and HOMA-IR values^[1].
Treatment with setmelanotide results in transient decreases in food intake (35%), with persistent weight loss over 8 weeks of treatment (13.5%) in a diet-induced obese nonhuman primate model^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 920014-72-8
Appearance Solid
Molecular Weight 1117.31
Formel C₄₉H₆₈N₁₈O₉S₂
Color White to off-white
Synonyms

RM-493; BIM-22493; IRC-022493
Sequence

Ac-Arg-Cys-{d-Ala}-His-{d-Phe}-Arg-Trp-Cys-NH2 (Disulfide bridge:Cys2-Cys8)
Sequence Shortening

Ac-RC-{d-Ala}-H-{d-Phe}-RWC-NH2 (Disulfide bridge:Cys2-Cys8)
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Sealed storage, away from moisture

Powder	-80°C	2 years
	-20°C	1 year

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Publications (8)

All In Vivo Efficacy StudyBio/Physico-chemical Assay

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Journal Impact Factor

Sci Transl Med

Orthopedia regulates melanocortin 4 receptor transcription and energy homeostasis. [Abstract]

2025 Jan 15;17(781):eadr6459. PMID: 39813316

Setmelanotide purchased from MedChemExpress. Usage Cited in: Sci Transl Med. 2025 Jan 15;17(781):eadr6459. [Abstract]

Setmelanotide (2 mg/kg; i.p.; once daily for 9 d) reduced body weights and food intake and improved glucose tolerance of HFD-fed OtpQ153R/+ mice, which quickly regained body weight after the treatment was discontinued.
J Exp Med

The atypical antipsychotic risperidone targets hypothalamic melanocortin 4 receptors to cause weight gain. [Abstract]

2021 Jul 5;218(7):e20202484. PMID: 33978701

Setmelanotide purchased from MedChemExpress. Usage Cited in: J Exp Med. 2021 Jul 5;218(7):e20202484. [Abstract]

Setmelanotide (100 nM) blocked the risperidone-induced hyperpolarization of MC4R^PVH neurons.

Setmelanotide purchased from MedChemExpress. Usage Cited in: J Exp Med. 2021 Jul 5;218(7):e20202484. [Abstract]

A single dose of Setmelanotide (SET) (2 mg/kg; i.p.) suppressed fast-induced refeeding in Mc4r^fl/fl mice.

Setmelanotide purchased from MedChemExpress. Usage Cited in: J Exp Med. 2021 Jul 5;218(7):e20202484. [Abstract]

Infusion of Setmelanotide (SET) (2 mg/kg; once daily for 14 d) attenuated hyperphagia in C57BL/6 mice fed with risperidone.

Setmelanotide purchased from MedChemExpress. Usage Cited in: J Exp Med. 2021 Jul 5;218(7):e20202484. [Abstract]

Setmelanotide (SET) (2 mg/kg; once daily for 14 d) caused accelerated glucose clearance of C57BL/6 mice fed with risperidone in a GTT.
Cell Rep

Melanocortin-4 receptors activate sympathetic preganglionic neurons and elevate blood pressure via TRPV1. [Abstract]

2022 Nov 1;41(5):111579. PMID: 36323255
J Med Chem

Click-Chemistry-Mediated Synthesis of Selective Melanocortin Receptor 4 Agonists. [Abstract]

2017 Nov 9;60(21):8716-8730. PMID: 28972753
Mol Metab

Lead-in calorie restriction enhances the weight-lowering efficacy of incretin hormone-based pharmacotherapies in mice. [Abstract]

2024 Sep 10:102027. PMID: 39265725
Front Immunol

Setmelanotide, a Novel, Selective Melanocortin Receptor-4 Agonist Exerts Anti-inflammatory Actions in Astrocytes and Promotes an Anti-inflammatory Macrophage Phenotype. [Abstract]

2019 Oct 4;10:2312. PMID: 31636637
J Clin Endocrinol Metab

MC4R variants modulate α-MSH and setmelanotide induced cellular signaling at multiple levels. [Abstract]

2024 Sep 16;109(10):2452-2466. PMID: 38567654
Charles University

2019 Jun.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (89.50 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 58.33 mg/mL (52.21 mM; Need ultrasonic)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

0.8950 mL

4.4750 mL

8.9501 mL

5 mM

0.1790 mL

0.8950 mL

1.7900 mL

10 mM

0.0895 mL

0.4475 mL

0.8950 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (2.24 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (2.24 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (2.24 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Working solution concentration: 0.22 mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact

MedChemExpress (MCE) .

Protokoll

Animal Administration^[1]

Mice: Mice are weighed. Baseline blood glucose is measured and 2 g/kg body weight of D-glucose injected by i.p. BIM-22493 is administered chronically at a dose of 300 nmol/kg/day for 14 days by sc. osmotic pump. Controls are administered with 0.9% saline during the same period. Blood glucose is measured at 15, 30, 60, and 120 minutes post injection^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (285 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Kumar KG, et al. Analysis of the therapeutic functions of novel melanocortin receptor agonists in MC3R- and MC4R-deficient C57BL/6J mice. Peptides. 2009 Oct;30(10):1892-900. [Content Brief]

[2]. Kievit P, et al. Chronic treatment with a melanocortin-4 receptor agonist causes weight loss, reduces resistance, and improves cardiovascular function in diet-induced obese rhesus macaques. Diabetes. 2013 Feb;62(2):490-7. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
H₂O / DMSO	1 mM	0.8950 mL	4.4750 mL	8.9501 mL	22.3752 mL
	5 mM	0.1790 mL	0.8950 mL	1.7900 mL	4.4750 mL
	10 mM	0.0895 mL	0.4475 mL	0.8950 mL	2.2375 mL
	15 mM	0.0597 mL	0.2983 mL	0.5967 mL	1.4917 mL
	20 mM	0.0448 mL	0.2238 mL	0.4475 mL	1.1188 mL
	25 mM	0.0358 mL	0.1790 mL	0.3580 mL	0.8950 mL
	30 mM	0.0298 mL	0.1492 mL	0.2983 mL	0.7458 mL
	40 mM	0.0224 mL	0.1119 mL	0.2238 mL	0.5594 mL
	50 mM	0.0179 mL	0.0895 mL	0.1790 mL	0.4475 mL
DMSO	60 mM	0.0149 mL	0.0746 mL	0.1492 mL	0.3729 mL
DMSO	80 mM	0.0112 mL	0.0559 mL	0.1119 mL	0.2797 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Keywords

Setmelanotide

8 Cited Publications

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Setmelanotide

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Publications Citing Use of MedChemExpress (MCE) Setmelanotide

Alle Melanocortin Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (8)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Setmelanotide

GPCR/G Protein Compound Library

Neuronal Signaling Compound Library

FDA-Approved Drug Library

Drug Repurposing Compound Library

Anti-diabetic Compound Library

Macrocyclic Compound Library

Endocrinology Compound Library

Anti-COVID-19 Compound Library

FDA Approved & Pharmacopeial Drug Library

Anti-Obesity Compound Library

Rare Diseases Drug Library

Peptide Library

Cyclic Peptide Library

Human Metabolite Library

Withdrawn Drug Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Activators Library

Bioactive Compound Library Max

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

FDA-Approved Drug Library Mini

Peptide Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

RNA Binding Bioactive Compound Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) Setmelanotide

Alle Melanocortin Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (8)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Setmelanotide Related Classifications

HY-19870 Related Classifications