research use only

Setmelanotide (RM-493) MC4R agonist

Cat.No.E1002

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.

Jump to

Quality Control

Batch: Purity: 99.76%
99.76

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (89.5 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 100 mg/mL

Ethanol : 100 mg/mL

Molarity Calculator

Mass Concentration Volume Molecular Weight
Dilution Calculator Molecular Weight Calculator

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg
g
μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO
%
% Tween 80
% ddH2O
% DMSO
+
%

Calculation results:

Working concentration: mg/ml;

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.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight 1117.31 Formula
C49H68N18O9S2
Storage (From the date of receipt) 3 years -20°C powder
CAS No. 920014-72-8 -- Storage of Stock Solutions

Synonyms BIM-22493, CAM 4072 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

Read more about storage stability stock solution CAS number SMILES

Mechanism of Action

Targets/IC50/Ki
MC4R
0.27 nM(EC50)
MC4R
2.1 nM(Ki)
In vitro

Setmelanotide (RM-493) decreases TNF-α/IFN-γ-induced chemokine expression in astrocytes and increases IL-6 and IL-11 mRNA and protein secretion via MC4R. It induces CREB phosphorylation in astrocytes, and this compound treated astrocytes secrete factors that are able to modulate macrophage polarization into an anti-inflammatory phenotype.

In vivo

Setmelanotide (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 this compound 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.

References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2026-06-29)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT07674290 RECRUITING
Bardet Biedl Syndrome (BBS); Bardet Biedl Syndrome; Bardet-Biedl Syndrome (BBS); Alstrom Syndrome
Tom Hühne
2023-01-01 PHASE4
NCT07496463 ENROLLING_BY_INVITATION
Pseudohypoparathyroidism Type 1a; Obesity
Massachusetts General Hospital
2026-07-21 PHASE2
NCT06760546 RECRUITING
Hypothalamic Obesity; Multiple Pituitary Hormone Deficiency Genetic Form; Septo-Optic Dysplasia; Optic Nerve Hypoplasia; Childhood-onset Combined Pituitary Hormone Deficiency; Pituitary Stalk Interruption Syndrome
Rhythm Pharmaceuticals, Inc.
2025-09-23 PHASE3
NCT06772597 ACTIVE_NOT_RECRUITING
Prader-Willi Syndrome; Obesity; Hyperphagia
Rhythm Pharmaceuticals, Inc.
2025-03-04 PHASE2
NCT06596135 COMPLETED
Obesity Associated With Defects in Leptin-melanocortin Pathway
Rhythm Pharmaceuticals, Inc.
2024-10-21 PHASE3
NCT05093634 COMPLETED
Obesity; Genetic Obesity
Rhythm Pharmaceuticals, Inc.
2021-12-10 PHASE3

Read more about Clinical Trials

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.