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Relamorelin

Product NameRelamorelin
CAS661472-41-9
MFC43H50N8O5S
MW790.98
EINECS
MOL File661472-41-9.mol

Chemical Properties

Boiling point	1216.171±65.00 °C(Press: 760.00 Torr)(predicted)
Density	1.361±0.10 g/cm3(Temp: 25 °C; Press: 760 Torr)(predicted)
pka	12.858±0.20(predicted)

Usage And Synthesis

Uses

Relamorelin (RM-131), a pentapeptide ghrelin analog, is a selective ghrelin/growth hormone secretagogue receptor (GHSR) agonist with a Ki of 0.42 nM for GHS-1a receptor. Relamorelin is centrally penetrant. Relamorelin increases growth hormone levels and accelerates gastric emptying. Relamorelin has the potential for cachexia, gastroparesis, and gastric/intestinal dysmobility disorders research[1][2][3][4].

in vivo

Relamorelin (RM-131; 50-500 nmol/kg/day; s.c.; continuous infusion for 5 days) decreases the loss of body mass and fat mass. Relamorelin (500 nmol/kg/day; continuous infusion for 5 days) increases the food intake and weight gain in rats^[1].
RM-131 (250-500nmol/kg; a single s.c.) stimulates acute food intake in wt but not growth hormone secretagogue receptor (GHR) ko mice^[2].

Animal Model:	F344/NTacfBR male rats implanted with tumor^[1]
Dosage:	50, 500 nmol/kg/day
Administration:	SC; continuous infusion at a rate of 0.5 μL/h for 5 d
Result:	Resulted in an increase in food intake (tumor/saline 41.4 g, tumor/BIM-28131 72.5 g) and weight gain (tumor/saline -10.3%, tumor/BIM-28131 +19.5%).

References

[1] DeBoer MD, et, al. Ghrelin treatment causes increased food intake and retention of lean body mass in a rat model of cancer cachexia. Endocrinology. 2007 Jun;148(6):3004-12. DOI:10.1210/en.2007-0016
[2] Fischer K, et, al. The Pentapeptide RM-131 Promotes Food Intake and Adiposity in Wildtype Mice but Not in Mice Lacking the Ghrelin Receptor. Front Nutr. 2015 Jan 12;1:31. DOI:10.3389/fnut.2014.00031
[3] Zatorski H, et, al. Relamorelin and other ghrelin receptor agonists - future options for gastroparesis, functional dyspepsia and proton pump inhibitors-resistant non-erosive reflux disease. J Physiol Pharmacol. 2017 Dec;68(6):797-805. PMID:29550791
[4] Matthew Heckroth, et al. Nausea and Vomiting in 2021: A Comprehensive Update. J Clin Gastroenterol. 2021 Apr 1;55(4):279-299. DOI:10.1097/MCG.0000000000001485
[5] Victor Chedid, et al. Relamorelin for the treatment of gastrointestinal motility disorders. Expert Opin Investig Drugs. 2017 Oct;26(10):1189-1197. DOI:10.1080/13543784.2017.1373088

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