920014-72-8
Chemical Structure
Setmelanotide
Synonym(s): RM-493; BIM-22493; IRC-022493
- CAS. Nr.: 920014-72-8
- Formula:C49H68N18O9S2
- Molecular Weight:1117.31
IUPAC Name: (4R,7S,10S,13R,16S,19R,22R)-16-((1H-imidazol-5-yl)methyl)-7-((1H-indol-3-yl)methyl)-22-((S)-2-acetamido-5-guanidinopentanamido)-13-benzyl-10-(3-guanidinopropyl)-19-methyl-6,9,12,15,18,21-hexaoxo-1,2-dithia-5,8,11,14,17,20-hexaazacyclotricosane-4-carboxamide
InChIKey: HDHDTKMUACZDAA-PHNIDTBTSA-N
SMILES: O=C(N[C@@H](CSSC[C@](C(N[C@@H]1C)=O)([H])NC([C@@H](NC(C)=O)CCCNC(N)=N)=O)C(N)=O)[C@@H](NC([C@@H](NC([C@@](NC([C@@H](NC1=O)CC2=CN=CN2)=O)([H])CC3=CC=CC=C3)=O)CCCNC(N)=N)=O)CC4=CNC5=CC=CC=C45
Biological Activity: Setmelanotide (RM-493) is a blood-brain barrier-permeable, selective MC4R agonist with a Ki value of 2.1 nM for hMC4R. Setmelanotide activates the CaMKK2/AMPK signaling pathway. Setmelanotide mediates body weight homeostasis, feeding regulation and energy expenditure modulation; it reduces food intake, induces weight loss, decreases obesity severity, increases daytime activity and energy expenditure, lowers levels of leptin, triglycerides, fasting insulin and diastolic blood pressure, improves insulin sensitivity, glucose tolerance and fatty liver condition, and reverses respiratory depression. Setmelanotide is applicable to research related to obesity, hyperinsulinemia, fatty liver and respiratory depression[1][2][3][4][5].
| Art. -Nr. | Produktname | Reinheit | Beschreibung | Pricing | |||||||||||||||||||
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Setmelanotide | 99.99% | Setmelanotide (RM-493) is a blood-brain barrier-permeable, selective MC4R agonist with a Ki value of 2.1 nM for hMC4R. Setmelanotide activates the CaMKK2/AMPK signaling pathway. Setmelanotide mediates body weight homeostasis, feeding regulation and energy expenditure modulation; it reduces food intake, induces weight loss, decreases obesity severity, increases daytime activity and energy expenditure, lowers levels of leptin, triglycerides, fasting insulin and diastolic blood pressure, improves insulin sensitivity, glucose tolerance and fatty liver condition, and reverses respiratory depression. Setmelanotide is applicable to research related to obesity, hyperinsulinemia, fatty liver and respiratory depression. | ||||||||||||||||||||
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References
- [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 insulin resistance, and improves cardiovascular function in diet-induced obese rhesus macaques. Diabetes. 2013;62(2):490-497. [Content Brief]
- [3]. Peng J, et al. Setmelanotide-mediated MC4R activation improves hypothalamic obesity via CaMKK2/AMPK pathways. Front Pharmacol. 2026;16:1730786. Published 2026 Jan 12. [Content Brief]
- [4]. Sharma S, et al. Current Mechanistic and Pharmacodynamic Understanding of Melanocortin-4 Receptor Activation. Molecules. 2019;24(10):1892. Published 2019 May 16. [Content Brief]
- [5]. Amorim MR, et al. Melanocortin receptor 4 agonist setmelanotide treats opioid-induced respiratory depression. bioRxiv [Preprint]. 2026 Mar 10:2026.03.08.708886. doi: 10.64898/2026.03.08.708886. PMID: 41959165; PMCID: PMC13061029. [Content Brief]
