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GH Axis · Reference monograph

Synthetic hexapeptide ghrelin-receptor agonist

Reference compound — not available from Purity Peptides. Shown for research context.

Overview

Hexarelin is a synthetic hexapeptide closely related to GHRP-6, differing by a methyl group on its D-tryptophan residue. That small change makes it one of the most potent growth hormone-releasing peptides described, and it was studied extensively by Italian endocrine groups during the 1990s.

Clinical research characterised its strong GH-releasing activity in adults and children and noted that responses tended to diminish with prolonged exposure, a phenomenon of partial desensitisation. Separately, animal studies uncovered cardiovascular activity that appeared independent of growth hormone, linked to binding at the scavenger receptor CD36 in heart tissue. These findings made hexarelin a reference compound for exploring non-pituitary actions of GH secretagogues. It has not been approved as a medicine and is prohibited in sport; we supply it exclusively for laboratory research.

Mechanism studied

  1. Hexarelin
  2. GHS-R1a & CD36
  3. GH release
  4. Cardiac signalling (preclinical)

Hexarelin activates GHS-R1a on pituitary and hypothalamic cells, raising intracellular calcium through Gq signalling and triggering GH release. Its potency exceeds that of GHRP-6 in most published comparisons. In cardiac tissue, hexarelin binds CD36, and rodent studies have reported improved function after ischaemia–reperfusion and reduced fibrosis, effects observed even in GH-deficient animals. With repeated exposure, the pituitary response attenuates, which has made hexarelin useful for studying receptor desensitisation and recovery.

Research highlights

  • 01Methylated GHRP-6 analogue with among the highest GH-releasing potency of its class
  • 02Clinical studies in the 1990s documented partial desensitisation with prolonged exposure
  • 03Binds cardiac CD36, with GH-independent effects reported in rodent heart models
  • 04Modest cortisol and prolactin increases reported alongside GH release
  • 05Prohibited in sport under WADA class S2

Latest published research

293 papers on PubMed →
  1. Histopathological and immunohistochemical characterization of MPTP-associated pancreatic injury and its attenuation by Hexarelin in mice

    Şahin M et al. · Journal of molecular histology · 2026 Sep 18 · PMID 42758352

  2. Protective and restorative effects of hexarelin on MPTP-induced lung injury in mice

    Celikoglu O et al. · Journal of basic and clinical physiology and pharmacology · 2026 Aug 21 · PMID 42619489

  3. The emerging landscape of performance-enhancing peptides modulating GH-IGF1 axis: bridging the gap between clinical evidence and patient self-administration

    Dominikowski A et al. · Frontiers in endocrinology · 2026 · PMID 42395176

  4. Hexarelin promotes the survival of retinal ganglion cells after optic nerve transection

    Chow KBS et al. · Indian journal of pharmacology · 2026 Mar 1 · PMID 41766237

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

    Pobee E et al. · Journal of analytical toxicology · 2025 Jul 1 · PMID 40465419

  6. Pharmacological targeting of the hyper-inflammatory response to SARS-CoV-2-infected K18-hACE2 mice using a cluster of differentiation 36 receptor modulator

    Gauvin J et al. · Frontiers in pharmacology · 2024 · PMID 38384295

  7. Revealing the interaction between peptide drugs and permeation enhancers in the presence of intestinal bile salts

    Hossain S et al. · Nanoscale · 2023 Dec 7 · PMID 37982184

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

    Guan C et al. · European journal of medical research · 2023 Sep 14 · PMID 37710348

Live feed from PubMed (NCBI) for “Hexarelin”, updated 2026-10-30. Listing a paper is not an endorsement of its findings.

Key references

  1. [1]Ghigo et al., 1997 — Eur J Endocrinol
  2. [2]PubMed — reviews on hexarelin
  3. [3]WADA — Prohibited List of Substances and Methods

FAQ

  • Animal studies show hexarelin binds the CD36 receptor in heart tissue and produces cardiovascular effects even without growth hormone. This makes it a useful tool for researchers investigating non-pituitary actions of GH secretagogues and the biology of CD36 signalling.

  • Lyophilized Hexarelin is normally kept sealed at −20 °C, protected from light and moisture. Once reconstituted for laboratory work, aliquots are held at 2–8 °C for short-term use or frozen, avoiding repeated freeze–thaw. Follow the lot-specific guidance on the certificate of analysis.

  • Every lot of Hexarelin ships with a certificate of analysis reporting HPLC purity, mass-spectrometry identity against the expected molecular weight, appearance and lot number. Match the COA lot to the vial label and keep it with your experimental records.

FOR RESEARCH USE ONLY.Not for human or veterinary use. Not intended to diagnose, treat, cure, or prevent any disease.

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