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Hexarelin

GH Secretagogue
ExamorelinEP-23905

Overview

Hexarelin, also known as Examorelin or EP-23905, is a synthetic hexapeptide growth hormone secretagogue. It is derived from the structure of GHRP-6, a peptide known for its ability to stimulate the release of growth hormone (GH). Hexarelin is synthesized through solid-phase peptide synthesis, a method that allows for the precise assembly of amino acids into a specific sequence. This compound has been of interest due to its potential applications in various medical and research fields. Researchers have primarily investigated Hexarelin for its effects on growth hormone release and its potential therapeutic applications. Studies have shown that Hexarelin can significantly increase GH levels in both animals and humans. It has been explored for its potential benefits in conditions such as growth hormone deficiency, cardiac dysfunction, and muscle wasting. Additionally, researchers have observed its cardioprotective effects, which may be beneficial in treating heart-related conditions. The mechanism of action of Hexarelin involves binding to the growth hormone secretagogue receptor (GHSR), a G-protein-coupled receptor. This interaction stimulates the pituitary gland to release growth hormone, mimicking the action of ghrelin, a natural hormone that regulates appetite and GH release. Hexarelin's pharmacokinetic properties include a relatively short half-life, with researchers noting a range of approximately 55 to 70 minutes when administered intravenously. It is known to have poor oral bioavailability, which limits its effectiveness when taken orally. The compound is more stable when administered via subcutaneous or intramuscular routes. Current research on Hexarelin is ongoing, with studies focusing on its potential therapeutic applications and long-term effects. However, it is not approved for medical use by major regulatory bodies, and its use is primarily confined to research settings. Regulatory standing varies by region, with some countries allowing its sale as a research chemical while others impose stricter controls.

Mechanism of Action

Hexarelin acts by binding to the growth hormone secretagogue receptor (GHSR), which is a G-protein-coupled receptor. This binding stimulates the release of growth hormone from the pituitary gland, mimicking the action of the endogenous hormone ghrelin.

Molecular Data

FormulaC47H58N12O6
Molecular Weight887 g/mol
CAS Number140703-51-1
PubChem CID6918297

Half-Life

SubcutaneousData limited
IntramuscularData limited
Intravenous~55 to 70 minutes
OralPoor bioavailability

Hexarelin's short half-life necessitates frequent administration for sustained effects.

Storage

Lyophilized

Stable for 2+ years at -20°C, 12 months at 4°C

Reconstituted

Use within 14 days when refrigerated at 4°C

Avoid

Avoid repeated freeze-thaw cycles, direct light

Solvent

Bacteriostatic water or sterile saline recommended

Solubility

Hexarelin is soluble in water and DMSO, but poorly soluble in acetonitrile.

Legal Status

🇩🇪DE

Not approved as a medicinal product. Not a controlled substance. Sale as research chemical is a legal grey area.

🇺🇸US

Not approved by the FDA for medical use. Not scheduled by the DEA.

🇦🇺AU

Not approved by the TGA for therapeutic use.

🇬🇧UK

Not approved by the MHRA for medical use.

Legal status information is provided for general reference only and may not reflect the most current regulatory changes. Always verify with official government sources before making any decisions.

9 Research Publications

Identification of alexamorelin consumption biomarkers using human hepatocyte incubations and high-resolution mass spectrometry.

Human

Journal of analytical toxicology · 2025

Researchers studied alexamorelin, a synthetic peptide that may enhance performance, to identify its consumption biomarkers for better doping control. They found that after processing in the liver, alexamorelin significantly decreased, with only one metabolite detected, which is not specific to alexamorelin use.

  • Researchers identified 21 potential metabolites of alexamorelin, with N-acetylation being the most likely transformation.
  • After incubating alexamorelin with liver cells, its levels dropped significantly, indicating rapid metabolism.
  • Only one metabolite, examorelin, was detected, but it is commercially available and not unique to alexamorelin consumption.
PubMed

Hexarelin alleviates apoptosis on ischemic acute kidney injury via MDM2/p53 pathway.

Animal

European journal of medical research · 2023

Researchers found that Hexarelin, a compound tested in rats, offers protection against acute kidney injury caused by reduced blood flow. The study observed that Hexarelin reduces cell death in kidney cells and improves kidney function by influencing specific proteins involved in the cell death process.

  • Hexarelin significantly mitigated kidney damage and improved function in a rat model of acute kidney injury.
  • The compound reduced cell death by altering the expression of key proteins related to apoptosis.
  • Molecular analysis suggested that Hexarelin interacts with MDM2, which plays a role in regulating cell survival.
PubMed

SARS-CoV-2 RNA Dependent RNA polymerase (RdRp) - A drug repurposing study.

Unknown

Heliyon · 2020

Researchers studied existing FDA-approved drugs to see if they could effectively interact with a key protein in the SARS-CoV-2 virus that helps it replicate. They found several drugs, including Ornipressin and Lypressin, that bind strongly to this protein, suggesting they could be potential candidates for further investigation in treating COVID-19.

  • Researchers observed that the crystal structure of the SARS-CoV-2 RNA Dependent RNA Polymerase (RdRp) was determined, revealing its reliance on specific viral cofactors.
  • The study screened 7,922 FDA-approved drugs and identified several that interact significantly with the active site of RdRp.
  • Notable candidates include Ornipressin and Lypressin, which showed strong binding within the RdRp's binding pockets.
PubMed

The CD36-PPARγ Pathway in Metabolic Disorders.

Review

International journal of molecular sciences · 2018

Researchers observed that the CD36-PPARγ pathway plays a significant role in regulating glucose and energy metabolism. They found that growth hormone releasing peptides (GHRP) can activate PPARγ, offering a new way to influence metabolic functions related to conditions like diabetes and atherosclerosis.

  • Researchers found that activating PPARγ can improve insulin resistance in diabetic patients.
  • The study identified GHRP as a potent activator of PPARγ through the scavenger receptor CD36.
  • Findings suggest that the GHRP-CD36-PPARγ pathway could help manage various metabolic disorders.
PubMed

Implications of ghrelin and hexarelin in diabetes and diabetes-associated heart diseases.

Review

Endocrine · 2015

Researchers reviewed the roles of ghrelin and its synthetic version, hexarelin, in diabetes and related heart diseases. They found that these compounds may help protect insulin-producing cells and improve glucose and fat metabolism, suggesting potential therapeutic benefits for diabetes management and heart health.

  • Researchers observed that ghrelin and hexarelin can enhance the regeneration of insulin-producing beta cells.
  • The study found that these compounds may improve glucose levels and insulin secretion.
  • Researchers noted that ghrelin and hexarelin have beneficial effects on cardiovascular health independent of growth hormone.
PubMed

The cardiovascular action of hexarelin.

Review

Journal of geriatric cardiology : JGC · 2014

Researchers observed that hexarelin, a synthetic peptide similar to ghrelin, may have direct effects on the heart and blood vessels, suggesting potential cardiovascular benefits. The study highlights hexarelin's stability and potency compared to ghrelin, indicating it could be a promising candidate for treating certain heart conditions.

  • Hexarelin activates growth hormone receptors in the brain and has direct cardiovascular effects.
  • It binds to a specific cardiac receptor, CD36, which mediates its protective effects on the heart.
  • Hexarelin is more stable and potent than its natural counterpart, ghrelin.
PubMed

We are ageing.

Review

BioMed research international · 2014

Researchers reviewed various theories and mechanisms related to ageing and longevity, highlighting the complexity of these processes. They found that factors like oxidative stress, metabolism, and inflammation play significant roles, with caloric restriction and specific biological pathways showing promise for promoting a longer life.

  • Researchers observed that multiple biological pathways, including those related to oxidative stress and metabolism, are involved in the ageing process.
  • The review identified caloric restriction and the target of rapamycin (TOR) as potential strategies for enhancing longevity.
  • Researchers noted that sirtuins and hormetic responses may also contribute to the understanding of ageing and longevity.
PubMed

Gateways to clinical trials.

Human

Methods and findings in experimental and clinical pharmacology · 2002

Researchers compiled a comprehensive guide to recent clinical trials involving various drugs, including treatments for conditions like HIV, cancer, and mental health disorders. This study highlights the ongoing research efforts and the wide range of medications currently being tested in clinical settings.

  • The guide includes information on numerous drugs such as adalimumab, metformin, and trastuzumab.
  • Researchers observed a focus on both established and emerging therapies across multiple health conditions.
  • The data was sourced from a specialized drug discovery and development portal, ensuring up-to-date information.
PubMed

Growth hormone-releasing peptides.

Review

European journal of endocrinology · 1997

Researchers reviewed growth hormone-releasing peptides (GHRPs), which are synthetic compounds that stimulate the release of growth hormone in both animals and humans. They found that GHRPs can effectively increase growth hormone levels through various mechanisms and have potential clinical applications for certain conditions related to growth hormone deficiency.

  • GHRPs have a significant and dose-related effect on growth hormone release, which persists even with different methods of administration.
  • The effectiveness of GHRPs varies with age, being highest in children and decreasing in older adults, but remains more potent than natural growth hormone-releasing hormone (GHRH).
  • GHRPs maintain their ability to stimulate growth hormone release in certain conditions, such as acromegaly and hyperthyroidism, but may be less effective in others like obesity and hypothyroidism.
PubMed

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This page is for informational and research purposes only. All information is based on published scientific literature. Nothing on this page constitutes medical advice or replaces consultation with a qualified healthcare professional.