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Relamorelin

MCE China：Relamorelin

Brand：MedChemExpress (MCE)

Cat. No.HY-19884

CAS：661472-41-9

Synonyms：RM-131; BIM-28131

Storage：Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping：Room temperature in continental US; may vary elsewhere.

Description：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.

In Vitro：Relamorelin (RM-131) shows ∼3 times greater affinity for GHS-1a (Ki=0.42 nM) than native ghrelin (Ki=1.12 nM). Relamorelin is 6 times more potent (EC50=0.71 nM) in activating the GHS-1a receptor than native ghrelin (EC50=4.2 nM) as assessed in vitro by calcium mobilization[1].

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 (250-500 nmol/kg; a single s.c.) stimulates acute food intake in wt but not growth hormone secretagogue receptor (GHR) ko mice[2].

IC50 & Target：Ki: 0.42 nM (GHS-1a)[1] In Vitro Relamorelin (RM-131) shows ∼3 times greater affinity for GHS-1a (Ki=0.42 nM) than native ghrelin (Ki=1.12 nM). Relamorelin is 6 times more potent (EC50=0.71 nM) in activating the GHS-1a receptor than native ghrelin (EC50=4.2 nM) as assessed in vitro by calcium mobilization[1]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> Relamorelin Related Antibodies

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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.  [Content Brief]

[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.  [Content Brief]

[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.  [Content Brief]

[4]. Matthew Heckroth, et al. Nausea and Vomiting in 2021: A Comprehensive Update. J Clin Gastroenterol. 2021 Apr 1;55(4):279-299.  [Content Brief]

[5]. Victor Chedid, et al. Relamorelin for the treatment of gastrointestinal motility disorders. Expert Opin Investig Drugs. 2017 Oct;26(10):1189-1197.  [Content Brief]