Relamorelin TFA

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Relamorelin TFA

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。

包装与价格：

包装	价格(元)
5mg	电议
10mg	电议
25mg	电议
50mg	电议
100mg	电议

产品名称

RM-131 TFA
BIM-28131 TFA

产品介绍

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。

生物活性

Relamorelin (RM-131) TFA, a pentapeptide ghrelin analog, is a selectiveghrelin/growth hormone secretagogue receptor (GHSR)agonist with aK_iof 0.42 nM forGHS-1areceptor. 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].

IC₅₀& Target

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

体外研究
(In Vitro)

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^[1].

体内研究
(In Vivo)

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].

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

905.00

性状

Solid

Formula

C₄₅H₅₁F₃N₈O₇S

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℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.
请依序添加每种溶剂： PBS
Solubility: 50 mg/mL (55.25 mM); Clear solution; Need ultrasonic

*以上所有助溶剂都可在本网站选购。