Relamorelin (RM-131) acetate, a pentapeptide ghrelin analog, is a selectiveghrelin/growth hormone secretagogue receptor (GHSR)agonist with aK_iof 0.42 nM forGHS-1areceptor. 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^{[1][2][3][4][5]}.

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

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 (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) 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].

851.02

C₄₅H₅₄N₈O₇S

1809080-14-5

Room temperature in continental US; may vary elsewhere.

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