keep away from moisture
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Setmelanotide (BIM-22493) is a selective agonist of melanocortin 4 receptor (MC4R)(human and rat MC4R with EC50s of 0.27 nM and 0.28 nM, respectively).
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | Inquiry | $ 87.00 | |
5 mg | Inquiry | $ 255.00 | |
10 mg | Inquiry | $ 398.00 | |
25 mg | Inquiry | $ 719.00 | |
50 mg | Inquiry | $ 1,164.00 | |
100 mg | Inquiry | $ 1,586.00 | |
1 mL * 10 mM (in DMSO) | Inquiry | $ 474.00 |
Description | Setmelanotide (BIM-22493) is a selective agonist of melanocortin 4 receptor (MC4R)(human and rat MC4R with EC50s of 0.27 nM and 0.28 nM, respectively). |
Targets&IC50 | MC4R (rat): 2.7 nM (ki), MC5R (human): 1600 nM (EC50), MC5R (human): 430 nM (ki), MC3R (human): 5.3nM (EC50), MC3R (human): 10 nM (ki), MC4R (rat):0.28 Nm (EC50), MC4R (human): 2.1 nM (ki), MC4R (human): 0.27 nM (EC50), MC1R (human):3.9 nM (ki), MC1R (human):5.8 nM (EC50) |
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)[1]. |
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[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]. |
Synonyms | BIM-22493, IRC-022493, RM-493 |
Molecular Weight | 1117.31 |
Formula | C49H68N18O9S2 |
CAS No. | 920014-72-8 |
keep away from moisture
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: 100 mg/mL (89.50 mM), Sonication is recommended.
DMSO: 100 mg/mL (89.50 mM), Sonication is recommended.
You can also refer to dose conversion for different animals. More
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Setmelanotide 920014-72-8 GPCR/G Protein Neuroscience Melanocortin Receptor BIM-22493 RM493 IRC 022493 IRC022493 BIM22493 RM 493 IRC-022493 BIM 22493 RM-493 inhibitor inhibit