Relamorelin TFA - KKL Med Inc.

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Relamorelin TFA

目录号 : KM15324

Data Sheet 产品使用指南

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 K_i 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。

规格	价格	是否有货
5mg		In-stock
10mg		In-stock
25mg		In-stock
50mg	询价	In-stock
100mg	询价	In-stock

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生物活性

Relamorelin (RM-131) TFA, a pentapeptide ghrelin analog, is a selective ghrelin/growth hormone secretagogue receptor (GHSR) agonist with a K_i 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.

体外研究

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

体内研究

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.
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.

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%).

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据

In Vitro:

H₂O : 100 mg/mL (110.50 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.1050 mL	5.5249 mL	11.0497 mL
5 mM	0.2210 mL	1.1050 mL	2.2099 mL
10 mM	0.1105 mL	0.5525 mL	1.1050 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-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。