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.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté : 99.16%
- CAS No.: 2863659-22-5
- Formule: C45H51F3N8O7S
- Masse moléculaire:905.00
-
Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Activité biologique
-
Chemical Information
-
Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
-
Help & FAQs
-
HY-14734A
Anamorelin hydrochlorideGhrelin Receptor Agonist -
HY-14820A
Macimorelin acetateGHSR Agonist -
HY-14734
AnamorelinGhrelin Receptor Agonist -
HY-U00433
JMV 2959 -
HY-50760
L-692585GHS-R1a Agonist -
HY-P0231
AZP-531Auxin Releases Peptide Analog -
HY-113906A
(αR,8aS)-GSK1614343Isomer of GSK1614343 -
HY-100579
Ferrostatin-1Ferroptosis Inhibitor -
HY-50844
Ibutamoren MesylateGHSR Agonist -
HY-15243
Capromorelin TartrateGHSR Agonist -
HY-13964
YIL781GHSR Antagonist -
HY-U00433A
JMV 2959 hydrochloride
Publications Citing Use of MedChemExpress (MCE) Relamorelin TFA
More
Activité biologique
Description
IC50 & Target
Ki: 0.42 nM (GHS-1a)[1]
In Vitro
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.
In Vivo
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.
-
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%).
Chemical Information
-
CAS No. 2863659-22-5
-
Appearance Solid
-
Masse moléculaire 905.00
-
Formule C45H51F3N8O7S
-
Color White to off-white
-
Synonyms
RM-131 TFA; BIM-28131 TFA
-
Livraison
Room temperature in continental US; may vary elsewhere.
-
Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (2)
-
Journal Impact Factor
-
Most Recent
-
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 -
Solvant et solubilité
In Vitro:
H2O : 100 mg/mL (110.50 mM; Need ultrasonic)
* 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.
* 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)
In Vivo:
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
Pureté et documentation
-
Fiche technique (282 KB)
-
SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
-
Instruction de manipulation (2659 KB)
Références
[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
| 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
Powered by Bioz