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Setmelanotide is a selective agonist of the MC4 receptor, with EC50 values of 0.27 nM and 0.28 nM for human and rat MC4R, respectively. Setmelanotide binds to and activates MC4 receptors in the paraventricular nucleus (PVN) of the hypothalamus and in the lateral hypothalamic area (LHA), areas involved in the regulation of appetite, and this action is thought to underlie its appetite suppressant effects. Setmelanotide increases resting energy expenditure in both obese animals and humans.
| Molecular Weight | 1117.31 |
| Formula | C49H68N18O9S2 |
| CAS Number | 920014-72-8 |
| Solubility (25°C) | Water ≥ 60 mg/mL DMSO ≥ 60 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Melanocortin Receptor Products |
|---|
| CRN04894
CRN04894 is an orally active MC2R antagonist that demonstrates in vivo efficacy in rat model of adrenocorticotropic hormone (ACTH)-stimulated corticosterone secretion. |
| BMS-470539
BMS-470539 is a synthetic MC-1R agonist with potent anti-inflammatory properties. |
| PF-00446687
PF-00446687 is a potent, selective melanocortin-4 receptor (MC4R) agonist with EC50 of 12 ± 1 nM. |
| BMS-470539 dihydrochloride
BMS-470539 dihydrochloride is a highly potent and selective melanocortin-1 receptor (MC-1R) agonist with an IC50 of 120 nM, an EC50 of 28 nM. |
| Undecylenoyl phenylalanine
Undecylenoyl phenylalanine is an antagonist for α-melanocyte-stimulating hormone (MSH) and β-adrenergic receptor (β-ADR) to reduce the melanogenesis in melanocytes. |
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