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Relamorelin acetate
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Relamorelin acetate图片
CAS NO:1809080-14-5
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品名称
RM-131 acetate
BIM-28131 acetate
产品介绍
Relamorelin (RM-131) acetate,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 acetate 是一种五肽,具有中枢渗透性。Relamorelin acetate 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。
生物活性

Relamorelin (RM-131) acetate, a pentapeptide ghrelin analog, is a selectiveghrelin/growth hormone secretagogue receptor (GHSR)agonist with aKiof 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].

IC50& Target

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

体外研究
(In Vitro)

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[1].

体内研究
(In Vivo)

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].

Animal Model:F344/NTacfBR male rats implanted with tumor[1]
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%).
Clinical Trial
分子量

851.02

Formula

C45H54N8O7S

CAS 号

1809080-14-5

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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