Relamorelin TFA
Based on 2 publication(s) in Google Scholar
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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.16%
- CAS 番号: 2863659-22-5
- 分子式: C45H51F3N8O7S
- 分子量:905.00
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保管条件:
Sealed storage, away from moisture.
Powder -80°C, 2 years , -20°C, 1 year* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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MedChemExpress（MCE）の使用を引用している文献 Relamorelin TFA
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生物活性
Ki: 0.42 nM (GHS-1a)[1]
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:F344/NTacfBR male rats implanted with tumor[1]
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Dosage:50, 500 nmol/kg/day
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Administration:SC; continuous infusion at a rate of 0.5 μL/h for 5 d
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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%).
化学情報
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CAS 番号 2863659-22-5
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性状 Solid
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分子量 905.00
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分子式 C45H51F3N8O7S
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Color White to off-white
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別名
RM-131 TFA; BIM-28131 TFA
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Sealed storage, away from moisture
Powder -80°C 2 years -20°C 1 year * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (2)
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Journal Impact Factor
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Most Recent
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Brain Res
Electroacupuncture treatment enhances hippocampal growth hormone level and restores mitochondrial function in vascular dementia rats. [Abstract]2026 Jun 26:1888:150444. PMID: 42361950 -
溶剤 & 溶解度
H2O : 100 mg/mL (110.50 mM; Need ultrasonic)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: PBS
Solubility: 50 mg/mL (55.25 mM); Clear solution; Need ultrasonic
純度とドキュメンテーション
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データシート (282 KB)
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- Portuguese - PT (393 KB)
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取扱説明書 (2659 KB)
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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
[4]. Matthew Heckroth, et al. Nausea and Vomiting in 2021: A Comprehensive Update. J Clin Gastroenterol. 2021 Apr 1;55(4):279-299. [Content Brief]
[5]. Victor Chedid, et al. Relamorelin for the treatment of gastrointestinal motility disorders. Expert Opin Investig Drugs. 2017 Oct;26(10):1189-1197. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O | 1 mM | 1.1050 mL | 5.5249 mL | 11.0497 mL | 27.6243 mL |
| 5 mM | 0.2210 mL | 1.1050 mL | 2.2099 mL | 5.5249 mL | |
| 10 mM | 0.1105 mL | 0.5525 mL | 1.1050 mL | 2.7624 mL | |
| 15 mM | 0.0737 mL | 0.3683 mL | 0.7366 mL | 1.8416 mL | |
| 20 mM | 0.0552 mL | 0.2762 mL | 0.5525 mL | 1.3812 mL | |
| 25 mM | 0.0442 mL | 0.2210 mL | 0.4420 mL | 1.1050 mL | |
| 30 mM | 0.0368 mL | 0.1842 mL | 0.3683 mL | 0.9208 mL | |
| 40 mM | 0.0276 mL | 0.1381 mL | 0.2762 mL | 0.6906 mL | |
| 50 mM | 0.0221 mL | 0.1105 mL | 0.2210 mL | 0.5525 mL | |
| 60 mM | 0.0184 mL | 0.0921 mL | 0.1842 mL | 0.4604 mL | |
| 80 mM | 0.0138 mL | 0.0691 mL | 0.1381 mL | 0.3453 mL | |
| 100 mM | 0.0110 mL | 0.0552 mL | 0.1105 mL | 0.2762 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Relamorelin TFA 関連分類
HY-19884B 関連分類
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