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

Cat. No.: HY-19870 Purity: 99.35%
Handling Instructions

Setmelanotide (RM-493;BIM-22493;IRC-022493) is a melanocortin 4 receptor (MC4R) agonist with an EC50 of 0.27 nM for human MC4R.

For research use only. We do not sell to patients.
Setmelanotide Chemical Structure

Setmelanotide Chemical Structure

CAS No. : 920014-72-8

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 737 In-stock
1 mg USD 132 In-stock
5 mg USD 396 In-stock
10 mg USD 600 In-stock
50 mg USD 1800 In-stock
100 mg USD 2520 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

Setmelanotide (RM-493;BIM-22493;IRC-022493) is a melanocortin 4 receptor (MC4R) agonist with an EC50 of 0.27 nM for human MC4R.

IC50 & Target

EC50:3.9 nM (hMC1R), 10 nM (hMC3R), 2.1 nM (hMC4R)[1] Ki: 5.8 nM (hMC1R), 5.3nM (hMC3R), 0.27 nM (hMC4R)[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
References
Preparing Stock Solutions
Concentration Volume 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.
Kinase Assay
[1]

Cell membranes are prepared from CHO-K1 cells stably expressing the human melanocortin receptor subtypes (MC1R, MC3R, MC4R and MC5R). They are incubated at 1-10 μg protein/well in 50 mM Tris-HCl, pH 7.4, containing 0.2% BSA, 5 mM MgCl2, 1 mM CaCl2 and 0.1 mg/mL bacitracin, with increasing concentrations of setmelanotide and 0.1-0.3 nM [125I]-NDP-α-MSH for 90-120 min at 37°C, depending on the receptor subtype. Bound from free [125I]-NDP-α-MSH is separated by filtration through GF/C glass fiber filters presoaked with 0.1 % (w/v) PEI. Filters are washed three times with 50 mM Tris-HCl, pH 7.4, at 0-4°C and assayed for radioactivity using Perkin Elmer Topcount scintillation counter[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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
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

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

H2O: ≥ 24 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Product Name:
Setmelanotide
Cat. No.:
HY-19870
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