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

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

Cat. No.: HY-19870 Purity: 99.00%
SDS COA Handling Instructions

Molarity Calculator

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.

Custom Peptide Synthesis

Setmelanotide Chemical Structure

Setmelanotide Chemical Structure

CAS No. : 920014-72-8

Size Price Stock
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 608 Ask For Quote & Lead Time
Solution
10 mM * 1 mL in DMSO USD 608 Ask For Quote & Lead Time
Solid
5 mg USD 396 Ask For Quote & Lead Time
10 mg USD 495 Ask For Quote & Lead Time
50 mg USD 880 Ask For Quote & Lead Time
100 mg USD 1500 Ask For Quote & Lead Time

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Other Forms of Setmelanotide:

Setmelanotide Related Antibodies

Top Publications Citing Use of Products

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MC1R MC3R MC2R MC4R MC5R

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

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. 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].

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

Setmelanotide Related Antibodies
In Vivo

Inhibition of refeeding after an overnight fast by Setmelanotide 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 glucose and HOMA-IR values[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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

1117.31

Formula

C49H68N18O9S2
CAS No.
Appearance

Solid

Color

White to off-white

Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Sealed storage, away from moisture

Powder -80°C 2 years
-20°C 1 year

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (89.50 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 62.5 mg/mL (55.94 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 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

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 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

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation

Purity: 99.82%

SDS (393 KB)

COA (260 KB) RP-HPLC (255 KB) MS (69 KB)

Handling Instructions (2659 KB)
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

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 0.8950 mL 4.4750 mL 8.9501 mL 22.3752 mL
5 mM 0.1790 mL 0.8950 mL 1.7900 mL 4.4750 mL
10 mM 0.0895 mL 0.4475 mL 0.8950 mL 2.2375 mL
15 mM 0.0597 mL 0.2983 mL 0.5967 mL 1.4917 mL
20 mM 0.0448 mL 0.2238 mL 0.4475 mL 1.1188 mL
25 mM 0.0358 mL 0.1790 mL 0.3580 mL 0.8950 mL
30 mM 0.0298 mL 0.1492 mL 0.2983 mL 0.7458 mL
40 mM 0.0224 mL 0.1119 mL 0.2238 mL 0.5594 mL
50 mM 0.0179 mL 0.0895 mL 0.1790 mL 0.4475 mL
DMSO 60 mM 0.0149 mL 0.0746 mL 0.1492 mL 0.3729 mL
80 mM 0.0112 mL 0.0559 mL 0.1119 mL 0.2797 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Setmelanotide Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Setmelanotide920014-72-8RM-493 BIM-22493 IRC-022493RM493RM 493BIM22493BIM 22493BIM-22493IRC022493IRC 022493IRC-022493Melanocortin ReceptorMC ReceptorInhibitorinhibitorinhibit

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