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 |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related Melanocortin Receptor Products |
|---|
| Adrenocorticotropic Hormone (ACTH) (4-10), human
Adrenocorticotropic Hormone (ACTH) (4-10), human is a melanocortin 4 (MC4R) receptor agonist. |
| γ1-MSH
γ1-MSH is a melanocortin MC3 receptor agonist, with a Ki of 34 nM for the rat MC3 receptor. |
| γ-1-Melanocyte Stimulating Hormone (MSH), amide
γ-1-Melanocyte Stimulating Hormone (MSH), amide is a 11-amino acid peptide. |
| JKC363
JKC363, a selective melanocortin MC4 receptor antagonist, has a 90-fold higher affinity at the MC4 receptor (IC50=0.5 nM) than at the MC3 receptor (44.9 nM). |
| ACTH (11-24)
ACTH (11-24) is an adrenocorticotropic hormone (ACTH) receptor antagonist. |
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