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.
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- Pureza: 99.16%
- No. CAS: 2863659-22-5
- Fòrmula: C45H51F3N8O7S
- Peso molecular:905.00
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Almacenamiento:
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)
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Publications Citing Use of MedChemExpress (MCE) Relamorelin TFA
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Actividad biológica
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%).
Chemical Information
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No. CAS 2863659-22-5
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Appearance Solid
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Peso molecular 905.00
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Fòrmula C45H51F3N8O7S
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Color White to off-white
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Synonyms
RM-131 TFA; BIM-28131 TFA
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
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 -
Solvente y solubilidad
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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
Pureza y Documentación
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Ficha de datos (282 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[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 Related Classifications
HY-19884B Related Classifications
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