Relamorelin

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Relamorelin (RM-131)，一种生长素类似物，是一种选择性的生长素释放肽/生长激素促分泌素受体 (GHSR) 激动剂，对 GHS-1a 受体的 Ki 值为 0.42 nM。Relamorelin 是一种五肽，具有中枢渗透性。Relamorelin 增加生长激素水平，加速胃排空，具有用于恶病质、胃轻瘫和胃/肠运动障碍研究的潜力。

Relamorelin (RM-131), 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 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.

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

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.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.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%).

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GPCR/G Protein

GHSR

GHSR

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661472-41-9

790.97

C43H50N8O5S

>98% (HPLC)

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C([C@@H](NC([C@@H](CC=1C=2C(SC1)=CC=CC2)NC(=O)C3CCNCC3)=O)C(N[C@H](C(NC4(C(N)=O)CCNCC4)=O)CC5=CC=CC=C5)=O)C=6C=7C(NC6)=CC=CC7

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(-20℃)

With Ice Pack

≥ 2 years