Formulation: A solid
Formal Name: cyclic (2→8)-disulfide N2-acetyl-L-arginyl-L-cysteinyl-D-alanyl-L-histidyl-D-phenylalanyl-L-arginyl-L-tryptophyl-L-cysteinamide, trifluoroacetate salt
Purity: ≥98%
Formula Markup: C49H68N18O9S2 • XCF3COOH
Formula Weight: 1117,3
Shelf life (days): 1460
Notes: Setmelanotide is a cyclic peptide agonist of melanocortin receptor 4 (MC4R).{66000} It increases cAMP production in CHO-K1 cells expressing MC4R, MC1R, MC3R, and MC5R (EC50s = 0.27, 5.8, 5.3, and 1,600 nM, respectively, for the human receptors) but not in cells expressing MC2R (EC50 = >10 µM). Setmelanotide (6.4 µmol/animal) inhibits food intake in MC3R, but not MC4R, knockout mice. It also reduces food intake and hepatosteatosis, induces weight loss, and decreases serum insulin, glucose, and leptin levels in a mouse model of diet-induced obesity when administered at a dose of 300 nmol/kg per day. Formulations containing setmelanotide have been used in chronic weight management due to proopiomelanocortin (POMC), proprotein convertase subtilisin/kexin type 1 (PCSK1), or leptin receptor deficiency.
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