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Setmelanotide Acetate(920014-72-8 free base)

Catalog No. T12882L CAS 2759937-80-7

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

Setmelanotide Acetate(920014-72-8 free base) (RM-493 Acetate) 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 Acetate(920014-72-8 free base) Chemical Structure

Setmelanotide Acetate(920014-72-8 free base), CAS 2759937-80-7

Pack Size	Availability	Price/USD
1 mg	In stock	$ 133.00
5 mg	In stock	$ 302.00
10 mg	In stock	$ 453.00
25 mg	In stock	$ 748.00
50 mg	In stock	$ 1,050.00
100 mg	In stock	$ 1,420.00
1 mL * 10 mM (in DMSO)	In stock	$ 585.00

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Purity: 100%

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Description	Setmelanotide Acetate(920014-72-8 free base) (RM-493 Acetate) 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), MC4R (rat):0.28 Nm (EC50), MC5R (human): 1600 nM (EC50), MC5R (human): 430 nM (ki), MC3R (human): 10 nM (ki), MC3R (human): 5.3nM (EC50), MC4R (human): 0.27 nM (EC50), MC4R (human): 2.1 nM (ki), 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	RM-493 Acetate, IRC-022493 Acetate, BIM-22493 Acetate
Molecular Weight	1177.35
Formula	C51H72N18O11S2
CAS No.	2759937-80-7

Storage

keep away from moisture

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

Solubility Information

DMSO: 22.5 mg/mL (19.11 mM)

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.

Related compound libraries

This product is contained In the following compound libraries：

Peptide Compound Library Drug Repurposing Compound Library Anti-Cancer Approved Drug Library Anti-Cancer Clinical Compound Library Anti-Cancer Drug Library Approved Drug Library FDA-Approved & Pharmacopeia Drug Library Cyclic Peptide Library Bioactive Compound Library Clinical Compound Library

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Keywords

Setmelanotide Acetate(920014-72-8 free base) 2759937-80-7 GPCR/G Protein Neuroscience Melanocortin Receptor RM 493 Acetate Setmelanotide Acetate(920014728 free base) BIM 22493 Acetate RM493 Acetate RM-493 Acetate BIM22493 Acetate IRC-022493 Acetate Setmelanotide Acetate(920014 72 8 free base) IRC022493 Acetate BIM-22493 Acetate IRC 022493 Acetate inhibitor inhibit

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