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1504602-49-6

1504602-49-6 structure
1504602-49-6 structure
  • Name: RM-493
  • Chemical Name: Setmelanotide acetate
  • CAS Number: 1504602-49-6
  • Molecular Formula: C49H68N18O9S2.xC2H4O2
  • Molecular Weight:
  • Catalog: Research Areas Endocrinology
  • Create Date: 2020-08-09 14:13:11
  • Modify Date: 2024-01-12 13:29:51
  • Setmelanotide acetate (RM-493 acetate) is a selective melanocortin 4 receptor (MC4R) agonist with EC50s of 0.27 nM and 0.28 nM for human and rat MC4R, respectively[1].
Name Setmelanotide acetate
Description Setmelanotide acetate (RM-493 acetate) is a selective melanocortin 4 receptor (MC4R) agonist with EC50s of 0.27 nM and 0.28 nM for human and rat MC4R, respectively[1].
Related Catalog
Target

Ki:3.9 nM (hMC1R), 10 nM (hMC3R), 2.1 nM (hMC4R), 430 nM (hMC5R), 2.7 nM (rMC4R)[1] EC50: 5.8 nM (hMC1R), 5.3nM (hMC3R), 0.27 nM (hMC4R), 0.28 (rMC4R), 1600 nM (hMC5R)[1]

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 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, and does not require MC3R. BIM-22493 acutely improves glucose homeostasis. Lepob/Lepob mice treated with BIM-22493 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].
References

[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.
Molecular Formula C49H68N18O9S2.xC2H4O2

Chemsrc provides CAS#:1504602-49-6 MSDS, density, melting point, boiling point, structure, formula, molecular weight, synthetic route, etc.
title: CAS No. 1504602-49-6 | Chemsrc address: https://m.chemsrc.com/en/baike/1566325.html

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