Relamorelin acetate(Synonyms: RM-131 acetate BIM-28131 acetate)

发表于由

Relamorelin acetate;(Synonyms: RM-131 acetate; BIM-28131 acetate)

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。

Relamorelin acetateamp;;(Synonyms: RM-131 acetate; BIM-28131 acetate)

Relamorelin acetate Chemical Structure

CAS No. : 1809080-14-5

规格 是否有货
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250 mg ; 询价 ;
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Relamorelin acetate 的其他形式现货产品:

Relamorelin TFA

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[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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.
参考文献

  • [1]. DeBoer MD, et, al. Ghrelin treatment causes increased food intake and retention of lean body mass in a rat model of cancer cachexia. Endocrinology. 2007 Jun;148(6):3004-12.

    [2]. Fischer K, et, al. The Pentapeptide RM-131 Promotes Food Intake and Adiposity in Wildtype Mice but Not in Mice Lacking the Ghrelin Receptor. Front Nutr. 2015 Jan 12;1:31.

    [3]. Zatorski H, et, al. Relamorelin and other ghrelin receptor agonists – future options for gastroparesis, functional dyspepsia and proton pump inhibitors-resistant non-erosive reflux disease. J Physiol Pharmacol. 2017 Dec;68(6):797-805.

    [4]. Matthew Heckroth, et al. Nausea and Vomiting in 2021: A Comprehensive Update. J Clin Gastroenterol. 2021 Apr 1;55(4):279-299.

    [5]. Victor Chedid, et al. Relamorelin for the treatment of gastrointestinal motility disorders. Expert Opin Investig Drugs. 2017 Oct;26(10):1189-1197.