Relamorelin (RM-131), a pentapeptide ghrelin analog, is a selectiveghrelin/growth hormone secretagogue receptor (GHSR)agonist with aK_iof 0.42 nM forGHS-1areceptor. 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].

Ki: 0.42 nM (GHS-1a)^[1]

Relamorelin (RM-131) shows ~3 times greater affinity for GHS-1a (K_i=0.42 nM) than native ghrelin (K_i=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].

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].

790.97

C₄₃H₅₀N₈O₅S

661472-41-9

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