Relamorelin;(Synonyms: RM-131; BIM-28131)
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 Chemical Structure
CAS No. : 661472-41-9
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Relamorelin 的其他形式现货产品:
生物活性 |
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[1][2][3][4]. |
IC50 Target |
Ki: 0.42 nM (GHS-1a)[1] |
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体外研究 (In Vitro) |
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[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only. |
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体内研究 (In Vivo) |
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]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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Clinical Trial |
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分子量 |
790.97 |
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Formula |
C43H50N8O5S |
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CAS 号 |
661472-41-9 |
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运输条件 |
Room temperature in continental US; may vary elsewhere. |
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储存方式 |
Please store the product under the recommended conditions in the Certificate of Analysis. |
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参考文献 |
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