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

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

Cat. No.: HY-19884B
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.

Relamorelin TFA Chemical Structure

Relamorelin TFA Chemical Structure

Size Price Stock Quantity
5 mg USD 420 In-stock
Estimated Time of Arrival: December 31
10 mg USD 650 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1450 In-stock
Estimated Time of Arrival: December 31
50 mg USD 2100 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2950 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 1 publication(s) in Google Scholar

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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].

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].

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%).
Molecular Weight

905.00

Formula

C₄₅H₅₁F₃N₈O₇S

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, sealed storage, away from moisture

*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
10 mM 0.1105 mL 0.5525 mL 1.1050 mL
*Please refer to the solubility information to select the appropriate solvent.
References
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Product Name:
Relamorelin TFA
Cat. No.:
HY-19884B
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