Description

Relamorelin (CAS 661472-41-9) is a synthetic pentapeptide analog of ghrelin, specifically designed to mimic the endogenous ghrelin hormone while enhancing receptor selectivity and pharmacokinetic stability. It functions primarily as a growth hormone secretagogue receptor (GHSR) agonist, demonstrating high affinity for the GHS-1a receptor with a Ki of 0.42 nM, indicating potent receptor activation at subnanomolar concentrations.

Relamorelin is capable of penetrating the central nervous system, allowing it to act both centrally and peripherally. In preclinical and translational studies, it has been shown to increase circulating growth hormone levels and stimulate gastric motility, accelerating gastric emptying. These effects make Relamorelin a valuable compound for laboratory research into disorders characterized by impaired gastrointestinal function, including gastroparesis, intestinal dysmotility, and conditions associated with cachexia or metabolic dysfunction.

The peptide’s pentapeptide structure confers both high receptor specificity and enhanced metabolic stability, ensuring reproducible biological activity in experimental models. In addition, Relamorelin’s pharmacological profile makes it a versatile tool for studies exploring ghrelin receptor signaling, hormone-mediated appetite regulation, and endocrine-motility interactions.

Relamorelin is supplied in lyophilized form, preserving stability and activity for laboratory use. GMP production ensures high purity and reproducibility, suitable for both wholesale and retail laboratory research applications.

For laboratory research use only. Not intended for human or veterinary use.

Product Specifications

Mechanism of Action & Research Applications

Relamorelin exerts its pharmacological effects primarily through activation of the growth hormone secretagogue receptor type 1a (GHSR-1a), which is abundantly expressed in both hypothalamic and peripheral tissues. Upon receptor binding, Relamorelin stimulates a cascade of intracellular events leading to enhanced growth hormone secretion from the anterior pituitary and modulation of gastrointestinal motility via central and enteric nervous system pathways.

Key Mechanisms

1. GHSR-1a Activation:
   Relamorelin binds selectively and potently to GHSR-1a, mimicking endogenous ghrelin’s effects. This receptor activation triggers intracellular signaling via G-protein-coupled pathways, leading to growth hormone release and modulation of gastrointestinal smooth muscle activity.

2. Central Nervous System Penetration:
   Unlike some peptide analogs, Relamorelin is centrally penetrant, allowing it to act on hypothalamic centers that regulate appetite, gastrointestinal motility, and growth hormone release. This CNS activity enables researchers to explore hormone-driven central mechanisms in metabolic and gastrointestinal studies.

3. Gastrointestinal Motility Acceleration:
   Relamorelin promotes gastric emptying and intestinal transit, making it a valuable tool for gastroparesis and dysmotility research. Mechanistic studies show modulation of vagal and enteric neurons, enhancing peristaltic activity and smooth muscle contractility.

4. Cachexia and Metabolic Disorder Research:
   By stimulating growth hormone release and modulating appetite-related pathways, Relamorelin is a useful experimental compound in cachexia, anorexia, and muscle-wasting studies, providing insights into potential therapeutic strategies for metabolic disorders.

5. Peptide Stability and Pharmacokinetics:
   The pentapeptide design confers improved metabolic stability relative to native ghrelin, allowing sustained receptor engagement in in vitro and in vivo studies. The lyophilized GMP-grade peptide ensures reproducibility and experimental reliability.

6. Applications in Translational Research:

   • Gastroparesis Models: Testing the effects on delayed gastric emptying.

   • Cachexia Studies: Investigating muscle wasting and weight-loss mechanisms.

   • Endocrinology Research: Exploring GH axis modulation and metabolic regulation.

   • Ghrelin Signaling Pathways: Studying CNS-mediated hormonal regulation.

Relamorelin is increasingly used in preclinical models, organoid systems, and ex vivo gastrointestinal preparations to explore therapeutic potential, mechanistic pathways, and peptide pharmacology. Its selective receptor activation and CNS penetration differentiate it from other ghrelin analogs, making it a leading research tool in endocrinology and gastrointestinal physiology.

Side Effects (For Reference in Research Models)

In laboratory research, Relamorelin is generally well-tolerated. Observed effects in model systems may include:

• Enhanced growth hormone levels: Must be monitored in endocrine studies to avoid confounding systemic effects.

• Accelerated gastrointestinal transit: May cause variability in ex vivo or in vivo motility assays.

• CNS-mediated behavioral changes: Due to central penetration, high doses may alter feeding or activity in animal models.

• Peptide stability considerations: Repeated freeze-thaw cycles can affect activity; use proper storage conditions.

• Experimental variability: Dose-dependent differences may require titration for reproducible outcomes.

Note: Relamorelin is intended solely for laboratory research. These observations are for experimental reference and do not represent clinical safety data.

Disclaimer

Relamorelin is supplied strictly for laboratory research purposes. It is not intended for human or veterinary use, nor as a therapeutic or dietary supplement. Users must follow standard laboratory safety procedures and storage recommendations.

Keywords

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• Cachexia and gastroparesis research

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