Setmelanotide Acetate(920014-72-8 free base)

SKU: orb1708547

Description

Setmelanotide Acetate(920014-72-8 free base)

Research Area

Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 2759937-80-7
• MW: 1177.35
• Purity: 100.00%
• 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);10% DMSO+40% PEG300+5% Tween-80+45% Saline:2 mg/mL (1.7 mM)

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. nM (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 sensitivit. 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 mode.
• 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 | Shipping with blue ice/Shipping at ambient temperature.
• Disclaimer: For research use only

Alternative Names

BIM22493 Acetate, BIM-22493 Acetate, BIM 22493 Acetate, hMC1R, hMC3R, hMC4R, hMC5R, MelanocortinReceptor, Melanocortin Receptor, IRC 022493 Acetate, IRC022493 Acetate, IRC-022493 Acetate, Setmelanotide Acetate(920014 72 8 free base), Setmelanotide Acetate(920014728 free base), Setmelanotide Acetate(920014-72-8 free base), RM 493 Acetate, RM493 Acetate, RM-493 Acetate, rMC4R

Compound Identifiers

PubChem CID

162341716