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Setmelanotide Acetate(920014-72-8 free base)

Catalog No. T12882L CAS T12882L

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

Setmelanotide 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), CAS T12882L

Pack Size	Availability	Price/USD
1 mg	In stock	$ 134.00
5 mg	In stock	$ 302.00
10 mg	In stock	$ 454.00
25 mg	In stock	$ 819.00
50 mg	In stock	$ 1,226.00
100 mg	In stock	$ 1,839.00

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Purity: 100%

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Description	Setmelanotide 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	hMC1R:3.9 nM (ki), hMC4R: 0.27 nM (EC50), hMC3R: 10 nM (ki), hMC5R: 1600 nM (EC50), rMC4R: 2.7 nM (ki), hMC1R:5.8 nM (EC50), hMC4R: 2.1 nM (ki), hMC3R: 5.3nM (EC50), hMC5R: 430 nM (ki), rMC4R:0.28 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 Acetate, RM-493 Acetate, IRC-022493 Acetate
Molecular Weight	1177.35
Formula	C51H72N18O11S2
CAS No.	T12882L

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 10 mM

( < 1 mg/ml refers to the product slightly soluble or insoluble )

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：

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

Related Products

Related compounds with same targets

HS 014 acetate(207678-81-7 free base) HS024 [D-Trp8]-γ-MSH acetate(321351-81-9 free base) Melanotan (MT)-II ACTH 11-24 acetate(4237-93-8 free base) α-MSH Adrenocorticotropic Hormone (ACTH) (4-10), human Bremelanotide Acetate

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Keywords

Setmelanotide Acetate(920014-72-8 free base) T12882L GPCR/G Protein Neuroscience Melanocortin Receptor BIM-22493 Acetate Setmelanotide Acetate(920014728 free base) RM-493 Acetate IRC-022493 Acetate Setmelanotide Acetate(920014 72 8 free base) Inhibitor inhibitor inhibit

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