Setmelanotide
Acetyl-RCaHfRWC-amide, Disulphide bridge Cys2-Cys8
Description
Application Data
Description
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Setmelanotide is a potent melanocortin receptor type 4 (MC4R) agonist. Administration leads to weight loss and is in trials as an obesity medication.
Application Data
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Data Sheet Material Safety Data Sheet (MSDS)Catalogue number crb1001533 Molecular Weight 1116.5 Sequence (one letter code) Acetyl-RCaHfRWC-amide, Disulphide bridge Cys2-Cys8
Sequence (three letter code) Acetyl-Arg-Cys-[D-Ala]-His-[D-Phe]-Arg-Trp-Cys-NH2 (Disulfide bridge: Cys2-Cys8)
Aliase RM 493, BIM 22493, IRC 022493 Modifications Disulfide bridge: Cys2-Cys8, where a is D-Ala, where f is D-Phe Purity >95% cas 920014-72-8 Storage -20°C References Clément et al., (2018). MC4R agonism promotes durable weight loss in patients with leptin receptor deficiency. Nature medicine, 24(5): 551. doi: 10.1038/s41591-018-0015-9.
Collet et al., (2017). Evaluation of a melanocortin-4 receptor (MC4R) agonist (Setmelanotide) in MC4R deficiency. Mol. Metab., 6(10): 1321. doi: 10.1016/j.molmet.2017.06.015.
Manufactured in: United Kingdom Pro-opiomelanocortin (POMC)-derived peptides act on neurons expressing the Melanocortin 4 receptor (MC4R) to reduce body weight. Setmelanotide is a highly potent MC4R agonist that leads to weight loss in diet-induced obese animals and obese individuals with complete POMC deficiency.
The endogenous ligand α-melanocyte-stimulating hormone (α-MSH) for MC4R has been shown to have a much lower affinity than Setmelanotide, explaining some of the drug’s potency. Administration of Setmelanotide to wildtype mice resulted in significant weight loss while MC4R knockout mice fail to respond. Setmelanotide is in numerous clinical trials and shows promising results. Patients with POMC defects upstream of MC4R show more significant responses to treatment than those with MC4R deficiency or obese controls.
