| Identification | Back Directory | [Name]
Irofulven | [CAS]
920014-72-8 | [Synonyms]
RM-493
BIM-22493
IRC-022493)
Setmelanodide
RM-493; BIM-22493; IRC-022493)
Ac-Arg-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-NH2
L-Cysteinamide, N2-acetyl-L-arginyl-L-cysteinyl-D-alanyl-L-histidyl-D-phenylalanyl-L-arginyl-L-tryptophyl-, cyclic (2→8)-disulfide | [EINECS(EC#)]
-0 | [Molecular Formula]
C49H68N18O9S2 | [MDL Number]
MFCD30532719 | [MOL File]
920014-72-8.mol | [Molecular Weight]
1117.32 |
| Chemical Properties | Back Directory | [density ]
1.54±0.1 g/cm3(Predicted) | [form ]
Solid | [pka]
12.82±0.70(Predicted) | [color ]
White to off-white | [Sequence]
Ac-Arg-Cys-D-Ala-His-D-Phe-Arg-Trp-Cys-NH2(Disulfide bond) | [InChIKey]
HDHDTKMUACZDAA-JFHGRQLZNA-N |
| Hazard Information | Back Directory | [Uses]
Setmelanotide (RM-493) 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]. | [in vivo]
Inhibition of refeeding after an overnight fast by Setmelanotide 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 glucose and HOMA-IR values[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. DOI:10.1016/j.peptides.2009.07.012
[2] Kievit P, et al. Chronic treatment with a melanocortin-4 receptor agonist causes weight loss, reduces resistance, and improves cardiovascular function in diet-induced obese rhesus macaques. Diabetes. 2013 Feb;62(2):490-7. DOI:10.2337/db12-0598 |
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