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Setmelanotide

Catalog No. T12882 CAS 920014-72-8

Synonyms: BIM-22493, IRC-022493, RM-493

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).

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Setmelanotide, CAS 920014-72-8

Pack Size	Availability	Price/USD
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

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Biological Description

Chemical Properties

Storage & Solubility Information

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

Storage

keep away from moisture

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: 100 mg/mL (89.50 mM), Sonication is recommended.

DMSO: 100 mg/mL (89.50 mM), Sonication is recommended.

References and Literature

1. Kumar KG, et al. Analysis of the therapeutic functions of novel melanocortin receptor agonists in MC3R- and MC4R-deficient C57BL/6J mice. Peptides. 2009 Oct;30(10):1892-900. 2. Kievit P, et al. Chronic treatment with a melanocortin-4 receptor agonist causes weight loss, reduces insulin resistance, and improves cardiovascular function in diet-induced obese rhesus macaques. Diabetes. 2013 Feb;62(2):490-7.

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Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

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

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