1. GPCR/G Protein
  2. GHSR
  3. Relamorelin TFA

Relamorelin TFA  (Synonyms: RM-131 TFA; BIM-28131 TFA)

Cat. No.: HY-19884B Purity: 99.89%
COA Handling Instructions

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.

For research use only. We do not sell to patients.

Custom Peptide Synthesis

Relamorelin TFA Chemical Structure

Relamorelin TFA Chemical Structure

CAS No. : 2863659-22-5

Size Price Stock Quantity
5 mg USD 420 In-stock
10 mg USD 650 In-stock
25 mg USD 1450 In-stock
50 mg USD 2100 In-stock
100 mg USD 2950 In-stock
200 mg   Get quote  
500 mg   Get quote  

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Relamorelin TFA:

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  • Biological Activity

  • Purity & Documentation

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Description

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[1][2][3][4][5].

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

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[1].
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%).
Clinical Trial
Molecular Weight

905.00

Formula

C45H51F3N8O7S

CAS No.
Appearance

Solid

Color

White to off-white

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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)

Solvent & Solubility
In Vitro: 

H2O : 100 mg/mL (110.50 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the 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.

* 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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.

  • Protocol 1

    Add each solvent one by one:  PBS

    Solubility: 50 mg/mL (55.25 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation
References

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.

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Relamorelin TFA Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
Relamorelin TFA
Cat. No.:
HY-19884B
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