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Hexarelin

Examorelin · EP-23905

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

Hexarelin is a synthetic growth hormone-releasing peptide that belongs to the class of growth hormone secretagogues (GHS), designed to stimulate the release of growth hormone from the pituitary gland. Researchers primarily study hexarelin for its potential roles in promoting longevity, cardiovascular health, and metabolic regulation. Key findings indicate that hexarelin not only enhances growth hormone release but also exerts direct cardioprotective effects through specific receptors in the heart, suggesting a multifaceted role in cardiovascular physiology. Additionally, studies suggest that hexarelin may influence insulin sensitivity and lipid metabolism, highlighting its relevance in diabetes and related complications. Current research continues to explore its safety, efficacy, and broader therapeutic applications in various clinical contexts.

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 acts primarily through the growth hormone secretagogue receptor (GHSR), stimulating growth hormone (GH) release via the activation of the phospholipase C (PLC) signaling pathway, which leads to increased intracellular calcium levels and subsequent GH secretion. Additionally, hexarelin interacts with the non-GHSR receptor CD36, mediating cardioprotective effects through pathways such as peroxisome proliferator-activated receptor gamma (PPAR-γ) regulation, influencing lipid metabolism and insulin sensitivity. While the exact mechanisms of action are not fully understood, hexarelin's effects extend beyond GH release, suggesting potential roles in cardiovascular protection and metabolic regulation.

Research

80 Research Publications

3,438

Total Citations

22

Human/RCT

3.1

Avg. Influence

2025

Latest

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#01

Growth hormone in obesity.

ReviewInfluence10.0
336
The study demonstrated that hexarelin elicits greater GH responses in obese patients compared to traditional stimuli, highlighting its potential role in obesity management.
1 microgram/kgintravenous(human)not mentioned2 microgram kg-1intravenous(human)not mentioned250 microg/kg s. c. twice dailysubcutaneous(dog)6 weeks25 micrograms/kgintravenous(rat)not mentioned10(-7) mol/lnot mentioned(rat)24 h4 microg/kg per hintravenous(rat)1.5 h
PubMed
#02

Central control of penile erection: role of the paraventricular nucleus of the hypothalamus.

AnimalInfluence3.0
218
Researchers observed that the paraventricular nucleus of the hypothalamus plays a crucial role in controlling erectile function in male rats through the activation of oxytocinergic neurons.
1 microgram/kgintravenous(human)not mentioned2 microgram kg-1intravenous(human)not mentioned250 microg/kg s. c. twice dailysubcutaneous(dog)6 weeks25 micrograms/kgintravenous(rat)not mentioned10(-7) mol/lnot mentioned(rat)24 h4 microg/kg per hintravenous(rat)1.5 h
PubMed
#03

Ghrelin regulates proliferation and differentiation of osteoblastic cells.

In VitroInfluence9.0
202
Researchers observed that both ghrelin and hexarelin significantly stimulated osteoblast proliferation and differentiation in rat calvarial osteoblast cultures, while EP-40737 showed an antiproliferative effect.
25 micrograms/kgi.v.(rat)not mentioned100 micrograms/hcontinuous infusion(rat)6, 30 or 174 h100 microgramsi.v.(human)not mentioned80 microgram/kg, b.i.d., s.c.s.c.(rat)30 days2 microgram kg-1i.v.(human)not mentioned250 micrograms/kgi.v.(dog)not mentioned
PubMed
#04

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 crucial for controlling erectile function and male sexual behavior in mammals.
1 microgram/kgintravenous(human)not mentioned2 microgram kg-1intravenous(human)not mentioned250 microg/kg s. c. twice dailysubcutaneous(dog)6 weeks25 micrograms/kgintravenous(rat)not mentioned10(-7) mol/lnot mentioned(rat)24 h4 microg/kg per hintravenous(rat)1.5 h
PubMed
#05

The CD36-PPARγ Pathway in Metabolic Disorders.

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

ReviewInfluence10.0
147
The study demonstrated that hexarelin activates PPARγ via CD36, suggesting its role 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.
1 microgram/kgintravenous(human)not mentioned2 microgram kg-1intravenous(human)not mentioned250 microg/kg s. c. twice dailysubcutaneous(dog)6 weeks25 micrograms/kgintravenous(rat)not mentioned10(-7) mol/lnot mentioned(rat)24 h4 microg/kg per hintravenous(rat)1.5 h
PubMed
#06

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

AnimalInfluence3.0
139
Researchers observed that hexarelin effectively stimulates GH secretion in both infant and adult rats, showing similar effectiveness to GHRP-6.
1 microgram/kgintravenous(human)not mentioned2 microgram kg-1intravenous(human)not mentioned250 microg/kg s. c. twice dailysubcutaneous(dog)6 weeks25 micrograms/kgintravenous(rat)not mentioned10(-7) mol/lnot mentioned(rat)24 h4 microg/kg per hintravenous(rat)1.5 h
PubMed
#07

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

In VitroInfluence2.0
118
Researchers observed that hexarelin stimulates cardiomyocyte proliferation in a dose-dependent manner, indicating its potential cardiovascular effects independent of GH secretion.
1 microgram/kgintravenous(human)not mentioned2 microgram kg-1intravenous(human)not mentioned250 microg/kg s. c. twice dailysubcutaneous(dog)6 weeks25 micrograms/kgintravenous(rat)not mentioned10(-7) mol/lnot mentioned(rat)24 h4 microg/kg per hintravenous(rat)1.5 h
PubMed
#08

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

AnimalInfluence5.0
115
The study demonstrated that hexarelin induces a dose-dependent increase in coronary perfusion pressure in rat hearts, suggesting a specific cardiac receptor's involvement.
2 microgram kg-1intravenous(human)25 micrograms/kgintravenous(rat)5 micrograms/kgintravenous(rat)80 micrograms/kg, b.i.d. s.c.subcutaneous(rat)100 micrograms/hcontinuous infusion(rat)6, 30 or 174 h
PubMed
#09

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
#10

Growth hormone-releasing peptides and their analogs.

ReviewInfluence2.0
95
Researchers observed that growth hormone-releasing peptides, including hexarelin, effectively stimulate GH release in both animals and humans through specific receptors in the pituitary and hypothalamus.
1 microgram/kgintravenous(human)not mentioned2 microgram kg-1intravenous(human)not mentioned250 microg/kg s. c. twice dailysubcutaneous(dog)6 weeks25 micrograms/kgintravenous(rat)not mentioned10(-7) mol/lnot mentioned(rat)24 h4 microg/kg per hintravenous(rat)1.5 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 regarding its potential impact on cancer incidence and mortality. Additionally, the exact mechanisms by which hexarelin exerts its cardioprotective effects via the non-GHSR CD36 receptor remain unclear, warranting further investigation.

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
  • Research Peptides UKUK
    2mg
    $12.64
    Price/mg
    $6.32/mg
  • Geo PeptidesUS
    5mg
    $32.99
    Price/mg
    $6.60/mg
  • Ruo BioUS
    5mg
    $34.00
    Price/mg
    $6.80/mg
  • MoglabsUS
    5mg
    $38.00
    Price/mg
    $7.60/mg

Top 5 of 24 offers from 21 vendors. Prices updated daily.

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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