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Relamorelin acetate

Relamorelin acetate

产品编号 T39236   CAS 1809080-14-5
别名: Relamorelin acetate, RM-131 acetate, BIM-28131acetate

Relamorelin (RM-131) acetate is a pentapeptide ghrelin analog that acts as a selective agonist for the ghrelin/growth hormone secretagogue receptor (GHSR). It exhibits a high affinity for the GHS-1a receptor, with a Ki value of 0.42 nM. Notably, Relamorelin acetate can cross the blood-brain barrier and target the central nervous system. This compound effectively increases growth hormone levels and promotes faster gastric emptying. Due to these properties, Relamorelin acetate holds promise for its potential applications in research related to cachexia, gastroparesis, and gastric/intestinal dysmobility disorders [4] [5].

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Relamorelin acetate Chemical Structure
Relamorelin acetate, CAS 1809080-14-5
规格 价格/CNY 货期 数量
25 mg ¥ 10,600 待询

Relamorelin acetate 的其他形式现货产品:

Relamorelin
其他形式的 Relamorelin acetate:
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
重组蛋白限时优惠
产品目录号及名称: Relamorelin acetate (T39236)
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参考文献
产品描述 Relamorelin (RM-131) acetate is a pentapeptide ghrelin analog that acts as a selective agonist for the ghrelin/growth hormone secretagogue receptor (GHSR). It exhibits a high affinity for the GHS-1a receptor, with a Ki value of 0.42 nM. Notably, Relamorelin acetate can cross the blood-brain barrier and target the central nervous system. This compound effectively increases growth hormone levels and promotes faster gastric emptying. Due to these properties, Relamorelin acetate holds promise for its potential applications in research related to cachexia, gastroparesis, and gastric/intestinal dysmobility disorders [4] [5].
靶点活性 GHS-1a:0.42 nM (Ki)
体外活性 Relamorelin (RM-131) acetate shows ~3 times greater affinity for GHS-1a (K i =0.42 nM) than native ghrelin (K i =1.12 nM). Relamorelin acetate is 6 times more potent (EC 50 =0.71 nM) in activating the GHS-1a receptor than native ghrelin (EC 50 =4.2 nM) as assessed in vitro by calcium mobilization[1].
体内活性 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]. 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%).
别名 Relamorelin acetate, RM-131 acetate, BIM-28131acetate
分子量 851.04
分子式 C45H54N8O7S
CAS No. 1809080-14-5

存储

keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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TargetMol Library Books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.

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Keywords

Relamorelin acetate 1809080-14-5 RM131 Acetate Relamorelin Acetate RM 131 Acetate RM-131 acetate BIM-28131acetate RM-131 Acetate Inhibitor inhibitor inhibit

 

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