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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 (GHRP) that stimulates the secretion of growth hormone by activating specific receptors in the pituitary and hypothalamus. Researchers primarily study hexarelin for its potential roles in regulating growth hormone levels, as well as its cardiovascular and metabolic effects. Key findings indicate that hexarelin not only enhances growth hormone release but also exhibits cardioprotective properties and influences lipid metabolism, suggesting a broader physiological impact beyond its endocrine functions. Current research is focused on elucidating its mechanisms of action and exploring its therapeutic applications in conditions such as obesity, diabetes, and cardiovascular diseases.

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), which is a G-protein-coupled receptor, leading to the activation of signaling pathways that promote growth hormone (GH) release from the pituitary gland. Additionally, hexarelin engages non-GHSR receptors such as CD36 in cardiac tissues, mediating cardioprotective effects and influencing pathways like peroxisome proliferator-activated receptor gamma (PPAR-γ) in adipocytes, which are involved in lipid metabolism and insulin sensitization. Although its GH-releasing mechanism is well-established, other aspects of hexarelin's actions, particularly its cardiovascular effects, are not fully understood.

Research

110 Research Publications

3,924

Total Citations

36

Human/RCT

2.7

Avg. Influence

2025

Latest

Sort
Filter
#01

Growth hormone in obesity.

ReviewInfluence10.0
336
The study found that hexarelin elicits greater GH responses in obese patients compared to GHRH, although responses remain lower than in lean subjects.
1 microgram/kgintravenous(human)25 micrograms/kgintravenous(rat)100 micrograms/hcontinuous infusion(rat)6, 30 or 174 h250 microg/kg s. c. twice dailysubcutaneous(dog)6 weeks10 microgintravenous(human)2 microgram kg-1intravenous(human)
PubMed
#02

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

ReviewInfluence4.0
219
Researchers observed that the paraventricular nucleus of the hypothalamus plays a crucial role in controlling penile erection and sexual behavior in male rats.
1 microgram/kgintravenous(human)25 micrograms/kgintravenous(rat)100 micrograms/hcontinuous infusion(rat)6, 30 or 174 h250 microg/kg s. c. twice dailysubcutaneous(dog)6 weeks10 microgintravenous(human)2 microgram kg-1intravenous(human)
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.

ReviewInfluence6.0
159
The study demonstrated that oxytocinergic neurons in the paraventricular nucleus are activated by hexarelin analogues to facilitate penile erection in male rats.
1 microgram/kgintravenous(human)25 micrograms/kgintravenous(rat)100 micrograms/hcontinuous infusion(rat)6, 30 or 174 h250 microg/kg s. c. twice dailysubcutaneous(dog)6 weeks10 microgintravenous(human)2 microgram kg-1intravenous(human)
PubMed
#05

The CD36-PPARγ Pathway in Metabolic Disorders.

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

ReviewInfluence10.0
150
The review indicated that hexarelin activates the CD36-PPARγ pathway, providing a novel approach to regulate 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)25 micrograms/kgintravenous(rat)100 micrograms/hcontinuous infusion(rat)6, 30 or 174 h250 microg/kg s. c. twice dailysubcutaneous(dog)6 weeks10 microgintravenous(human)2 microgram kg-1intravenous(human)
PubMed
#06

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 a prolonged effect following subcutaneous administration.
1 microgram/kgintravenous(human)25 micrograms/kgintravenous(rat)100 micrograms/hcontinuous infusion(rat)6, 30 or 174 h250 microg/kg s. c. twice dailysubcutaneous(dog)6 weeks10 microgintravenous(human)2 microgram kg-1intravenous(human)
PubMed
#07

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

In VitroInfluence2.0
119
The study demonstrated that hexarelin stimulates cardiomyocyte proliferation in H9c2 cells, suggesting a direct effect on cardiac cell growth.
1 microgram/kgintravenous(human)25 micrograms/kgintravenous(rat)100 micrograms/hcontinuous infusion(rat)6, 30 or 174 h250 microg/kg s. c. twice dailysubcutaneous(dog)6 weeks10 microgintravenous(human)2 microgram kg-1intravenous(human)
PubMed
#08

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

AnimalInfluence5.0
115
The study demonstrated the presence of a new hexarelin receptor in rat hearts, suggesting its role in regulating coronary vascular tone through specific binding interactions.
1 microgram/kgintravenous(human)not specified250 microg/kg s. c. twice dailysubcutaneous(dog)6 weeks2 microg/kgintravenous(human)not specified25 micrograms/kgintravenous(rat)not specified100 micrograms/hnot specified(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 hormone combined with arginine or growth hormone secretagogues for the diagnosis of growth hormone deficiency in adults.

HumanInfluence3.0
95
The study demonstrated that combining GHRH with arginine or hexarelin provides a reliable diagnostic test for adult growth hormone deficiency.
1 microgram/kgintravenous(human)not mentioned20 micrograms/kgintranasal(human)not mentioned2.0 micrograms/kg i.v.intravenous(human)not mentioned0.3 mg/kg/dayintravenous(mouse)21 days200 μg/kg body weightintraperitoneal(mouse)12 days
PubMed
Safety

Safety & Handling

Research Gaps

The specific long-term effects of hexarelin on cardiovascular health and metabolic regulation in humans remain unclear, as there is a lack of extensive human trials assessing its chronic administration. Additionally, the precise mechanisms by which hexarelin exerts its GH-independent effects, particularly in the context of insulin sensitivity and beta cell regeneration, have not been fully elucidated.

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

48 total
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Pricing

Price Comparison

  • BESTRCpeptidesEU
    10mg
    $54.00
    Price/mg
    $5.40/mg
  • bulkpeptidesupply.comUS
    5mg
    $27.50
    Price/mg
    $5.50/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

Top 5 of 29 offers from 25 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