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编 号：F747252
分子式：C45H54N8O7S
分子量：851.02
分子式：C45H54N8O7S
分子量：851.02
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CAS No: 1809080-14-5
产品详情
生物活性：
Relamorelin (RM-131) acetate, 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 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.
体内研究：
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.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.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%).
体外研究：
Relamorelin (RM-131) acetate shows ～3 times greater affinity for GHS-1a (Ki=0.42 nM) than native ghrelin (Ki=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.
Relamorelin (RM-131) acetate, 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 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.
体内研究：
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.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.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%).
体外研究：
Relamorelin (RM-131) acetate shows ～3 times greater affinity for GHS-1a (Ki=0.42 nM) than native ghrelin (Ki=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.
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