Relamorelin TFA (C09-1167-427)

Relamorelin (RM-131) TFA, 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 TFA is centrally penetrant. Relamorelin TFA increases growth hormone levels and accelerates gastric emptying. Relamorelin TFA has the potential for cachexia, gastroparesis, and gastric/intestinal dysmobility disorders researchIn VitroRelamorelin (RM-131) TFA shows ∼3 times greater affinity for GHS-1a (K i =0.42 nM) than native ghrelin (K i =1.12 nM). Relamorelin TFA 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.In VivoRelamorelin (RM-131; 50-500 nmol/kg/day; s.c.; continuous infusion for 5 days) TFA decreases the loss of body mass and fat mass. Relamorelin (500 nmol/kg/day; continuous infusion for 5 days) TFA increases the food intake and weight gain in rats . RM-131 (250-500 nmol/kg; a single s.c.) TFA stimulates acute food intake in wt but not growth hormone secretagogue receptor (GHR) ko mice. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: F344/NTacfBR male rats implanted with tumor 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%).Form:SolidIC50& Target:Ki: 0.42 nM (GHS-1a). Specifications and Purity: 99%. Molecular Formula: C45H51F3N8O7S. Molecular Weight: 905.00.