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Relamorelin acetate

Catalog No. T39236 CAS 1809080-14-5

Synonyms: Relamorelin acetate, RM-131 acetate, BIM-28131acetate

Relamorelin (RM-131) acetate is a pentapeptide ghrelin analog that acts as a selective agonist for the ghrelin/growth hormone secretagogue receptor (GHSR). It exhibits a high affinity for the GHS-1a receptor, with a Ki value of 0.42 nM. Notably, Relamorelin acetate can cross the blood-brain barrier and target the central nervous system. This compound effectively increases growth hormone levels and promotes faster gastric emptying. Due to these properties, Relamorelin acetate holds promise for its potential applications in research related to cachexia, gastroparesis, and gastric/intestinal dysmobility disorders [4] [5].

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Relamorelin acetate, CAS 1809080-14-5

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Description	Relamorelin (RM-131) acetate is a pentapeptide ghrelin analog that acts as a selective agonist for the ghrelin/growth hormone secretagogue receptor (GHSR). It exhibits a high affinity for the GHS-1a receptor, with a Ki value of 0.42 nM. Notably, Relamorelin acetate can cross the blood-brain barrier and target the central nervous system. This compound effectively increases growth hormone levels and promotes faster gastric emptying. Due to these properties, Relamorelin acetate holds promise for its potential applications in research related to cachexia, gastroparesis, and gastric/intestinal dysmobility disorders [4] [5].
Targets&IC50	GHS-1a:0.42 nM (Ki)
In vitro	Relamorelin acetate, also known as RM-131, exhibits approximately threefold higher affinity for the GHS-1a receptor (K i = 0.42 nM) compared to native ghrelin (K i = 1.12 nM). Furthermore, it is sixfold more potent (EC 50 = 0.71 nM) in activating the GHS-1a receptor than native ghrelin (EC 50 = 4.2 nM), as demonstrated by in vitro calcium mobilization assays[1].
In vivo	Relamorelin (RM-131; 50-500 nmol/kg/day; subcutaneously [s.c.] via continuous infusion for 5 days) acetate effectively reduces the loss of both body and fat mass. At a dosage of 500 nmol/kg/day administered subcutaneously through continuous infusion over a 5-day period, relamorelin acetate notably enhances food consumption and promotes weight gain in rats[1]. Furthermore, RM-131 (250-500 nmol/kg; single s.c. dose) acetate has been demonstrated to acutely increase food intake in wild-type mice, but this effect is not observed in mice lacking growth hormone secretagogue receptor (GHR) [2]. This research utilized F344/NTacfBR male rats implanted with tumors as the animal model[1], with dosages administered at 50 and 500 nmol/kg/day, subcutaneously, at a continuous infusion rate of 0.5 μL/h for 5 days. The outcomes revealed a significant increment in food intake (comparing tumor/saline at 41.4g with tumor/BIM-28131 at 72.5g) and an increase in weight (from tumor/saline -10.3% to tumor/BIM-28131 +19.5%).

Synonyms	Relamorelin acetate, RM-131 acetate, BIM-28131acetate
Molecular Weight	851.04
Formula	C45H54N8O7S
CAS No.	1809080-14-5

Storage

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Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

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. 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. 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. 4. Matthew Heckroth, et al. Nausea and Vomiting in 2021: A Comprehensive Update. J Clin Gastroenterol. 2021 Apr 1;55(4):279-299. 5. Victor Chedid, et al. Relamorelin for the treatment of gastrointestinal motility disorders. Expert Opin Investig Drugs. 2017 Oct;26(10):1189-1197.

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Keywords

Relamorelin acetate 1809080-14-5 RM131 Acetate Relamorelin Acetate RM 131 Acetate RM-131 acetate BIM-28131acetate RM-131 Acetate inhibitor inhibit

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