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Hexarelin

Examorelin · EP-23905

GH SecretagoguePreclinical
From$5.40/mgCompare prices
MW
887g/mol
Formula
C47H58N12O6

Hexarelin is a synthetic hexapeptide classified as a growth hormone-releasing peptide (GHRP), designed to stimulate the secretion of growth hormone (GH) from the pituitary gland. Researchers primarily study hexarelin for its potential roles in growth hormone regulation and its broader physiological effects, including cardiovascular and metabolic functions. Key findings indicate that hexarelin not only promotes GH release but also exhibits cardioprotective properties through its action on specific receptors in the heart, suggesting a role in cardiovascular health. Additionally, studies have highlighted its potential influence on glucose metabolism and insulin sensitivity, particularly in the context of diabetes and associated complications. Current research continues to explore the multifaceted effects of hexarelin, aiming to better understand its mechanisms and potential therapeutic applications in various clinical scenarios.

Chemical Profile

Chemical Profile

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

Half-Life

SCSubcutaneous

Data limited

IMIntramuscular

Data limited

IVIntravenous

~55 to 70 minutes

POOral

Poor bioavailability

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

Mechanism

Mechanism of Action

Hexarelin primarily acts by binding to the growth hormone secretagogue receptor (GHSR) in the brain and peripheral tissues, leading to the activation of signaling pathways such as the phosphatidylinositol-3 kinase (PI3K)/protein kinase B (Akt) pathway, which mediates its growth hormone-releasing effects and cardioprotective actions. Additionally, hexarelin interacts with the non-GHSR receptor CD36, contributing to its cardiovascular benefits through modulation of lipid metabolism and insulin sensitivity. While its mechanisms are partially understood, further research is needed to fully elucidate all pathways involved in its diverse biological effects.

Research

69 Research Publications

2,702

Total Citations

20

Human/RCT

3.0

Avg. Influence

2025

Latest

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#01

Growth hormone in obesity.

AnimalInfluence10.0
336
Researchers observed that hexarelin elicits growth hormone responses in obese patients that are greater than those evoked by GHRH, although still lower than those in lean subjects.
2 microgram/kgintravenous(human)25 micrograms/kgintravenous(rat)80 micrograms/kgsubcutaneous(rat)3, 5 or 10 days100 micrograms/hcontinuous infusion(rat)6, 30 or 174 h10(-7) mol/l(rat)24 h
PubMed
#02

The role of oxytocin and the paraventricular nucleus in the sexual behaviour of male mammals.

AnimalInfluence6.0
158
Researchers observed that oxytocinergic neurons in the paraventricular nucleus are activated by hexarelin analogs to facilitate male sexual behavior in rats.
1 microgram/kgintravenous(human)1 microgintracerebroventricular(rat)10 microgintravenous(human)2.0 microg/kgintravenous(human)25 micrograms/kgintravenous(rat)100 μg/kgsubcutaneous(rat)30 days330 μg/kgintraperitoneal(rat)5 microg/kgintravenous(rat)50 microg/m2/hintravenous(human)
PubMed
#03

The CD36-PPARγ Pathway in Metabolic Disorders.

Maréchal Loïze, et al. · International journal of molecular sciences · 2018

ReviewInfluence10.0
141
The review summarized that hexarelin activates PPARγ via the CD36 pathway, suggesting its potential in regulating lipid and energy metabolism in metabolic disorders.

Key findings

  1. 01Researchers found that activating PPARγ can improve insulin resistance in diabetic patients.
  2. 02The study identified GHRP as a potent activator of PPARγ through the scavenger receptor CD36.
  3. 03Findings suggest that the GHRP-CD36-PPARγ pathway could help manage various metabolic disorders.
2 microgram/kgintravenous(human)25 micrograms/kgintravenous(rat)80 micrograms/kgsubcutaneous(rat)3, 5 or 10 days100 micrograms/hcontinuous infusion(rat)6, 30 or 174 h10(-7) mol/l(rat)24 h
PubMed
#04

GH-releasing activity of Hexarelin, a new growth hormone releasing peptide, in infant and adult rats.

AnimalInfluence3.0
139
The study demonstrated that hexarelin effectively stimulates growth hormone secretion in both infant and adult rats, with variations in response based on age and GHRH function.
2 microgram/kgintravenous(human)25 micrograms/kgintravenous(rat)80 micrograms/kgsubcutaneous(rat)3, 5 or 10 days100 micrograms/hcontinuous infusion(rat)6, 30 or 174 h10(-7) mol/l(rat)24 h
PubMed
#05

Natural (ghrelin) and synthetic (hexarelin) GH secretagogues stimulate H9c2 cardiomyocyte cell proliferation.

In VitroInfluence2.0
118
Researchers observed that hexarelin stimulates cardiomyocyte proliferation in H9c2 cells, indicating its potential peripheral effects on the cardiovascular system independent of GH secretion.
2 microgram/kgintravenous(human)25 micrograms/kgintravenous(rat)80 micrograms/kgsubcutaneous(rat)3, 5 or 10 days100 micrograms/hcontinuous infusion(rat)6, 30 or 174 h10(-7) mol/l(rat)24 h
PubMed
#06

Identification and characterization of a new growth hormone-releasing peptide receptor in the heart.

AnimalInfluence5.0
115
The study demonstrated that hexarelin binds to a specific receptor in the heart, inducing vasoconstriction and suggesting a novel cardiac receptor's role.
2 microgram/kgintravenous(human)25 micrograms/kgintravenous(rat)80 micrograms/kgsubcutaneous(rat)3, 5 or 10 days100 micrograms/hcontinuous infusion(rat)6, 30 or 174 h10(-7) mol/l(rat)24 h
PubMed
#07

The growth hormone secretagogue hexarelin stimulates the hypothalamo-pituitary-adrenal axis via arginine vasopressin.

HumanInfluence4.0
101
The study demonstrated that hexarelin stimulates the hypothalamo-pituitary-adrenal axis in humans, likely through the release of arginine vasopressin.
1 microgram/kgintravenous(human)1 microgintracerebroventricular(rat)10 microgintravenous(human)2.0 microg/kgintravenous(human)25 micrograms/kgintravenous(rat)100 μg/kgsubcutaneous(rat)30 days330 μg/kgintraperitoneal(rat)5 microg/kgintravenous(rat)50 microg/m2/hintravenous(human)
PubMed
#08

Growth hormone-releasing peptides and their analogs.

ReviewInfluence2.0
96
Researchers observed that growth hormone-releasing peptides, including hexarelin, stimulate growth hormone release through specific receptors, with potential therapeutic implications in various conditions.
2 microgram/kgintravenous(human)25 micrograms/kgintravenous(rat)80 micrograms/kgsubcutaneous(rat)3, 5 or 10 days100 micrograms/hcontinuous infusion(rat)6, 30 or 174 h10(-7) mol/l(rat)24 h
PubMed
#09

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

Ahmad Jamshaid, et al. · Heliyon · 2020

ReviewInfluence8.0
89
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.

Key findings

  1. 01Researchers observed that the crystal structure of the SARS-CoV-2 RNA Dependent RNA Polymerase (RdRp) was determined, revealing its reliance on specific viral cofactors.
  2. 02The study screened 7,922 FDA-approved drugs and identified several that interact significantly with the active site of RdRp.
  3. 03Notable candidates include Ornipressin and Lypressin, which showed strong binding within the RdRp's binding pockets.
PubMed
#10

Arginine and growth hormone-releasing hormone restore the blunted growth hormone-releasing activity of hexarelin in elderly subjects.

Human
88
The study demonstrated that the GH response to hexarelin is significantly greater in young subjects compared to elderly subjects, with arginine enhancing the response in the elderly but not in the young.
2 microgram/kgintravenous(human)25 micrograms/kgintravenous(rat)80 micrograms/kgsubcutaneous(rat)3, 5 or 10 days100 micrograms/hcontinuous infusion(rat)6, 30 or 174 h10(-7) mol/l(rat)24 h
PubMed
Safety

Safety & Handling

Research Gaps

No long-term, rigorously controlled studies have been conducted to evaluate the safety and efficacy of hexarelin in diverse clinical scenarios, particularly concerning cancer incidence and mortality. Additionally, the precise mechanisms underlying hexarelin's actions, especially its synergistic effects with GHRH and the implications of repeated administration on GH responsivity, remain unclear.

Solubility

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

Storage & Handling

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

Safety information is derived from published research and may not reflect all known risks. This is not medical advice.

Legal Status

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.

Community Insights

Community Insights

Publications per Year

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Pricing

Price Comparison

  • BESTRCpeptidesEU
    10mg
    $54.00
    Price/mg
    $5.40/mg
    View
  • Research Peptides UKUK
    2mg
    $12.64
    Price/mg
    $6.32/mg
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  • Geo PeptidesUS
    5mg
    $32.99
    Price/mg
    $6.60/mg
    View
  • Ruo BioUS
    5mg
    $36.00
    Price/mg
    $7.20/mg
    View
  • MoglabsUS
    5mg
    $38.00
    Price/mg
    $7.60/mg
    View

Top 5 of 26 offers from 23 vendors. Prices updated daily.

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Mechanism

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Mechanism

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Legal Disclaimer

This page is for informational and research purposes only. All information is based on published scientific literature and does not constitute medical advice, diagnosis, or treatment recommendations. Many substances listed may not be approved for human use and may be subject to drug regulation laws (e.g., AMG in Germany, FDA in the US). PepStack does not encourage the use of any substance on humans. Always consult a qualified healthcare professional before making any health-related decisions. Use of this information is entirely at your own risk. PepStack assumes no liability for the accuracy, completeness, or timeliness of the content provided. Full disclaimer