| Name | Setmelanotide |
| 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. |
| 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]. |
| Storage | Keep away from moisture | 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.
10% DMSO+40% PEG300+5% Tween-80+45% Saline : 3.3 mg/mL (2.95 mM), Sonication is recommended.
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| Keywords | Setmelanotide | rMC4R | RM 493 | MelanocortinReceptor | Melanocortin Receptor | IRC 022493 | hMC5R | hMC4R | hMC3R | hMC1R | BIM 22493 |
| Inhibitors Related | (±)-Eriodictyol | α-MSH | 4-Methyl-6-Methoxycoumarin | Fenoprofen Calcium | α-MSH acetate | Afamelanotide acetate | BMS-470539 dihydrochloride | ACTH (1-17) acetate | Tetracosactide acetate | [D-Trp8]-γ-MSH acetate(321351-81-9 free base) | 2-MNG | Undecylenoyl phenylalanine |
| Related Compound Libraries | FDA-Approved & Pharmacopeia Drug Library | Bioactive Compound Library | Approved Drug Library | Neuronal Signaling Compound Library | Drug Repurposing Compound Library | Peptide Compound Library | Immunology/Inflammation Compound Library | Bioactive Compounds Library Max | GPCR Compound Library |
United States
