Relamorelin (RM-131) acetate, a pentapeptide ghrelin analog, is a selective ghrelin/growth hormone secretagogue receptor (GHSR) agonist with a K i of 0.42 nM for GHS-1a receptor. Relamorelin acetate is centrally penetrant. Relamorelin acetate increases growth hormone levels and accelerates gastric emptying. Relamorelin acetate has the potential for cachexia, gastroparesis, and gastric/intestinal dysmobility disorders research[4] [5] .

Relamorelin (RM-131) acetate shows ～3 times greater affinity for GHS-1a (K i =0.42 nM) than native ghrelin (K i =1.12 nM). Relamorelin acetate is 6 times more potent (EC 50 =0.71 nM) in activating the GHS-1a receptor than native ghrelin (EC 50 =4.2 nM) as assessed in vitro by calcium mobilization[1].

Relamorelin (RM-131; 50-500 nmol/kg/day; s.c.; continuous infusion for 5 days) acetate decreases the loss of body mass and fat mass. Relamorelin (500 nmol/kg/day; continuous infusion for 5 days) acetate increases the food intake and weight gain in rats[1]. RM-131 (250-500?nmol/kg; a single s.c.) acetate 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%).

1809080-14-5

C45H54N8O7S

851.04

BIM-28131acetate;Relamorelin acetate;RM-131 acetate;Relamorelin acetate

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years