1. GPCR/G Protein
    Neuronal Signaling
  2. Melanocortin Receptor
  3. Setmelanotide acetate

Setmelanotide acetate (Synonyms: RM-493 acetate; BIM-22493 acetate; IRC-022493 acetate)

Cat. No.: HY-19870B
Handling Instructions

Setmelanotide acetate (RM-493 acetate) is a selective melanocortin 4 receptor (MC4R) agonist with EC50s of 0.27 nM and 0.28 nM for human and rat MC4R, respectively.

For research use only. We do not sell to patients.

Custom Peptide Synthesis

Setmelanotide acetate Chemical Structure

Setmelanotide acetate Chemical Structure

CAS No. : 1504602-49-6

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Based on 2 publication(s) in Google Scholar

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Description

Setmelanotide acetate (RM-493 acetate) is a selective melanocortin 4 receptor (MC4R) agonist with EC50s of 0.27 nM and 0.28 nM for human and rat MC4R, respectively[1].

IC50 & Target

Ki:3.9 nM (hMC1R), 10 nM (hMC3R), 2.1 nM (hMC4R), 430 nM (hMC5R), 2.7 nM (rMC4R)[1]
EC50: 5.8 nM (hMC1R), 5.3nM (hMC3R), 0.27 nM (hMC4R), 0.28 (rMC4R), 1600 nM (hMC5R)[1]

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 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, and does not require MC3R. BIM-22493 acutely improves glucose homeostasis. Lepob/Lepob mice treated with BIM-22493 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].

Formula

C₄₉H₆₈N₁₈O₉S₂.xC₂H₄O₂

CAS No.

1504602-49-6

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

SetmelanotideRM-493BIM-22493IRC-022493RM493RM 493BIM22493BIM 22493IRC022493IRC 022493Melanocortin ReceptorMC ReceptorInhibitorinhibitorinhibit

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Setmelanotide acetate
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HY-19870B
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