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Relamorelin TFA Sale

(Synonyms: RM-131 TFA; BIM-28131 TFA) 目录号 : GC63727

Relamorelin (RM-131) TFA,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 TFA 是一种五肽,具有中枢渗透性。Relamorelin TFA 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 TFA Chemical Structure

Cas No.:2863659-22-5

规格 价格 库存 购买数量
5 mg
¥3,780.00
现货
10 mg
¥5,850.00
现货
25 mg
¥13,050.00
现货

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Sample solution is provided at 25 µL, 10mM.

产品文档

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产品描述

Relamorelin (RM-131) TFA, 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 TFA is centrally penetrant. Relamorelin TFA increases growth hormone levels and accelerates gastric emptying. Relamorelin TFA has the potential for cachexia, gastroparesis, and gastric/intestinal dysmobility disorders research[1][2][3][4][5].

Relamorelin (RM-131) TFA shows ∼3 times greater affinity for GHS-1a (Ki=0.42 nM) than native ghrelin (Ki=1.12 nM). Relamorelin TFA 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].

Relamorelin (RM-131; 50-500 nmol/kg/day; s.c.; continuous infusion for 5 days) TFA decreases the loss of body mass and fat mass. Relamorelin (500 nmol/kg/day; continuous infusion for 5 days) TFA increases the food intake and weight gain in rats[1].RM-131 (250-500 nmol/kg; a single s.c.) TFA stimulates acute food intake in wt but not growth hormone secretagogue receptor (GHR) ko mice[2].

[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.

Chemical Properties

Cas No. 2863659-22-5 SDF
别名 RM-131 TFA; BIM-28131 TFA
分子式 C45H51F3N8O7S 分子量 905
溶解度 Water : 100 mg/mL (110.50 mM; Need ultrasonic) 储存条件 -20°C, away from moisture
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
Shipping Condition 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。

溶解性数据

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1 mg 5 mg 10 mg
1 mM 1.105 mL 5.5249 mL 11.0497 mL
5 mM 0.221 mL 1.105 mL 2.2099 mL
10 mM 0.1105 mL 0.5525 mL 1.105 mL
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