Relamorelin TFA RM-131 TFA; BIM-28131 TFA|cas:2863659-22-5|西域试剂

Relamorelin TFA RM-131 TFA; BIM-28131 TFA,99.81%

产品编号：Bellancom-19884B| CAS NO：2863659-22-5| 分子式：C₄₅H₅₁F₃N₈O₇S| 分子量：905.00

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货号	价格	库存与货期
Bellancom-19884B	￥4200.00	杭州北京（现货）
Bellancom-19884B	￥6500.00	杭州北京（现货）
Bellancom-19884B	￥14500.00	杭州北京（现货）

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Relamorelin TFA 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 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^[4]^[5].

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.

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

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.

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

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%).

体内研究

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

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%).

性状

Solid

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。

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