Setmelanotide Acetate(920014-72-8 free base)

SKU: orb1708547

Description

Setmelanotide Acetate (RM-493 Acetate; 920014-72-8 free base) is a potent and selective MC4R agonist, demonstrating high activity in both human and rat receptors. It is a valuable research tool for studying energy homeostasis, obesity, and related metabolic disorders in preclinical in vitro and in vivo models.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 2759937-80-7
• MW: 1177.35
• Purity: >99% (May vary between batches)
• Formula: C₅₁H₇₂N₁₈O₁₁S₂
• SMILES: O=C([C@@H](NC([C@H](NC([C@@H](NC([C@H](NC([C@H](CSSC[C@H](NC1=O)C(N)=O)NC([C@@H](NC(C)=O)CCCNC(N)=N)=O)=O)C)=O)CC2=CN=CN2)=O)CC3=CC=CC=C3)=O)CCCNC(N)=N)N[C@H]1CC4=CNC5=CC=CC=C45.CC(O)=O
• Target: Melanocortin Receptor
• Solubility: DMSO: 22.5 mg/mL (19.11 mM), sonication is recommended.

Bioactivity

• Target IC50:
  MC4R (human): 0.27 nM (EC50)|MC4R (human): 2.1 nM (ki)|MC1R (human):3.9 nM (ki)|MC1R (human):5.8 nM (EC50)|MC3R (human): 10 nM (ki)|MC3R (human): 5.3nM (EC50)|MC4R (rat): 2.7 nM (ki)|MC4R (rat):0.28 Nm (EC50)|MC5R (human): 1600 nM (EC50)|MC5R (human): 430 nM (ki)
• 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. 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.
• 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).

Storage & Handling

• Storage: Keep away from moisture. Powder: -20°C for 3 years. In solvent: -80°C for 1 year.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

RM-493 Acetate, IRC-022493 Acetate, BIM-22493 Acetate

Compound Identifiers

PubChem CID

162341716