| Name | Setmelanotide Acetate(920014-72-8 free base) |
| Description | Setmelanotide Acetate(920014-72-8 free base) (RM-493 Acetate) is a selective agonist of melanocortin 4 receptor (MC4R)(human and rat MC4R with EC50s of 0.27 nM and 0.28 nM, respectively). |
| In vitro | Melanocortin receptor agonists act in the brain to regulate food intake and body weight and, independently of these actions, affect insulin sensitivity. Setmelanotide exhibits agonist activity to human and rat MC4R(human and rat MC4R with Kis of 2.1 and 2.7 nM and EC50s of 0.27 and 0.28 nM, respectively)[1]. |
| In vivo | Inhibition of refeeding after an overnight fast by BIM-22493 is dependent on functional MC4R.glucose homeostasis acutely improved by BIM-22493. BIM-22493(Lepob/Lepob mice) exhibits significantly improved glucose clearance when compared to controls. Chronic BIM-22493 treatment was associated with significantly lower levels of serum insulin, glucose and HOMA-IR values, suggesting an improvement in insulin sensitivity[1]. Treatment with setmelanotide results in transient decreases in food intake (35%), with persistent weight loss over 8 weeks of treatment (13.5%) in a diet-induced obese nonhuman primate model[2]. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween-80+45% Saline : 2 mg/mL (1.7 mM), Sonication is recommended.
DMSO : 22.5 mg/mL (19.11 mM), Sonication is recommended.
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| Keywords | Setmelanotide Acetate(920014-72-8 free base) | Setmelanotide Acetate(920014728 free base) | Setmelanotide Acetate(920014 72 8 free base) | rMC4R | RM493 Acetate | RM 493 Acetate | MelanocortinReceptor | Melanocortin Receptor | IRC022493 Acetate | IRC 022493 Acetate | hMC5R | hMC4R | hMC3R | hMC1R | BIM22493 Acetate | BIM 22493 Acetate |
| Inhibitors Related | (±)-Eriodictyol | α-MSH | 4-Methyl-6-Methoxycoumarin | Fenoprofen Calcium | α-MSH acetate | BMS-470539 dihydrochloride | Bremelanotide | ACTH (1-17) acetate | Tetracosactide acetate | 2-MNG | Undecylenoyl phenylalanine | Bremelanotide Acetate |
| Related Compound Libraries | Bioactive Compound Library | Cyclic Peptide Library | Membrane Protein-targeted Compound Library | Toxic Compound Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Peptide Compound Library | Anti-Cancer Approved Drug Library | FDA-Approved Drug Library | Bioactive Compounds Library Max | GPCR Compound Library | Anti-Cancer Drug Library |
United States
