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Irofulven

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Irofulven Basic information

Product Name:
Irofulven
Synonyms:
  • Setmelanodide
  • BIM-22493
  • IRC-022493)
  • RM-493
  • 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
  • Setmelanotide (RM-493) trifluoroacetate salt
CAS:
920014-72-8
MF:
C49H68N18O9S2
MW:
1117.32
EINECS:
000-000-0
Mol File:
920014-72-8.mol
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Irofulven Chemical Properties

Density 
1.54±0.1 g/cm3(Predicted)
pka
12.82±0.70(Predicted)
form 
Solid
color 
White to off-white
Sequence
Ac-Arg-Cys-D-Ala-His-D-Phe-Arg-Trp-Cys-NH2(Disulfide bond)
InChIKey
HDHDTKMUACZDAA-JFHGRQLZNA-N
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Irofulven Usage And Synthesis

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

IrofulvenSupplier

Zhejiang Jiekun Biotechnology Co., Ltd Gold
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0571-88211951 13735575465
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ShangHai Caerulum Pharma Discovery Co., Ltd.
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18149758185
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Wuxi Zhongkun Biochemical Technology Co., Ltd.
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0510-85629785 18013409632
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Hangzhou Peptide Biochem Co.,Ltd
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0571-89197072; 18668118770
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linda@peptide-china.com
Shanghai YuanYe Biotechnology Co., Ltd.
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021-61312847; 18021002903
Email
3008007409@qq.com
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