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

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

Cat. No.: HY-19870 Purity: 98.67%
Handling Instructions

Setmelanotide (RM-493) 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.

Setmelanotide Chemical Structure

Setmelanotide Chemical Structure

CAS No. : 920014-72-8

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5 mg USD 396 In-stock
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100 mg USD 1500 In-stock
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Customer Review

Based on 2 publication(s) in Google Scholar

Other Forms of Setmelanotide:

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Description

Setmelanotide (RM-493) 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].

Clinical Trial
Molecular Weight

1117.31

Formula

C₄₉H₆₈N₁₈O₉S₂

CAS No.

920014-72-8

SMILES

O=C(N[[email protected]@H](CSSC[[email protected]](C(N[[email protected]@H]1C)=O)([H])NC([[email protected]@H](NC(C)=O)CCCNC(N)=N)=O)C(N)=O)[[email protected]@H](NC([[email protected]@H](NC([[email protected]@](NC([[email protected]@H](NC1=O)CC2=CN=CN2)=O)([H])CC3=CC=CC=C3)=O)CCCNC(N)=N)=O)CC4=CNC5=CC=CC=C45

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

H2O : 100 mg/mL (89.50 mM; Need ultrasonic)

DMSO : 100 mg/mL (89.50 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.8950 mL 4.4750 mL 8.9501 mL
5 mM 0.1790 mL 0.8950 mL 1.7900 mL
10 mM 0.0895 mL 0.4475 mL 0.8950 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (2.24 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (2.24 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (2.24 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Animal Administration
[1]

Mice: Mice are weighed. Baseline blood glucose is measured and 2 g/kg body weight of D-glucose injected by i.p. BIM-22493 is administered chronically at a dose of 300 nmol/kg/day for 14 days by sc. osmotic pump. Controls are administered with 0.9% saline during the same period. Blood glucose is measured at 15, 30, 60, and 120 minutes post injection[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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Keywords:

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

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