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.
research use only
Cat.No.E1002
| Related Targets | CXCR Hedgehog/Smoothened PKA Adrenergic Receptor AChR 5-HT Receptor Histamine Receptor Dopamine Receptor Ras KRas |
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| Other Melanocortin Receptor Inhibitors | JNJ-10229570 α-MSH Bremelanotide Acetate |
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In vitro |
DMSO
: 100 mg/mL
(89.5 mM)
Water : 100 mg/mL Ethanol : 100 mg/mL |
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In vivo |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
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| Molecular Weight | 1117.31 | Formula | C49H68N18O9S2
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Storage (From the date of receipt) | 3 years -20°C powder |
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| CAS No. | 920014-72-8 | -- | Storage of Stock Solutions |
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| 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
| Targets/IC50/Ki |
MC4R
0.27 nM(EC50)
MC4R
2.1 nM(Ki)
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|---|---|
| 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 |
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(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 |
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