Hexarelin (Examorelin) is the most potent characterized GHRP hexapeptide — GHS-R1a agonist with Phase II human data and unique CD36 cardiac receptor binding providing GH-independent cardioprotection in animal models.
Product definition
What is Hexarelin Acetate?
Hexarelin (Examorelin) is the most potent characterized GHRP hexapeptide — GHS-R1a agonist with Phase II human data and unique CD36 cardiac receptor binding providing GH-independent cardioprotection in animal models.
Hexarelin (His-D-2-MeTrp-Ala-Trp-D-Phe-Lys-NH2; Examorelin) is a synthetic hexapeptide GH secretagogue developed by Europeptides SA (France) and licensed to Pharmacia for clinical development. The 2-MeTrp (2-methyltryptophan) substitution at position 2 relative to GHRP-6 is primarily responsible for the increased potency compared to the parent compound.
Phase I/II clinical development was conducted by Pharmacia for GH deficiency indications, producing published human pharmacokinetic data and dose-response characterization that is available in the research literature. Development was discontinued before regulatory submission for commercial reasons, leaving a compound with the most complete clinical pharmacokinetic characterization of any research GHRP that did not reach approval.
The CD36 binding was identified during mechanistic characterization of hexarelin's cardioprotective effects in animal ischemia models. CD36 is a class B scavenger receptor expressed on cardiomyocytes, macrophages, and endothelial cells. Hexarelin's GH-independent cardiac effects — reduced infarct size, preserved ejection fraction in myocardial ischemia models — have been attributed to CD36-mediated signaling rather than GHS-R1a activation, establishing hexarelin as a dual-receptor research tool.
Research context
How is Hexarelin Acetate described in the research literature?
Hexarelin activates GHS-R1a (ghrelin receptor) with the highest potency of any characterized GHRP hexapeptide, producing maximal GH release alongside cortisol and prolactin co-stimulation. Additionally binds CD36 scavenger receptor in cardiac tissue, producing GH-independent cardioprotective effects in ischemia models — a mechanistic dimension absent from all other GHRPs.
Compound profile
Key facts about Hexarelin Acetate
- Class
- Synthetic hexapeptide GHRP / GHS-R1a agonist (most potent characterized)
- Also known as
- Examorelin
- Amino acids
- 6
- Molecular weight
- ~888 Da
- CAS
- 140703-51-1
- Potency
- Highest GH release of any characterized GHRP hexapeptide
- Secondary receptor
- CD36 scavenger receptor — GH-independent cardiac effects
- Clinical status
- Phase II human data published; development discontinued pre-approval
- Research category
- GH secretagogue, GHS-R1a pharmacology, cardiac biology, CD36 receptor
- Storage
- Lyophilized: −20°C. Reconstituted: 2–8°C, use within 30 days
Research areas
What research areas is Hexarelin Acetate associated with?
- Most potent characterized GHRP hexapeptide — highest GH release per molar dose in direct comparison studies
- Phase II human pharmacokinetic data published — clinical characterization unusual for research-supply GHRP class
- Unique CD36 cardiac receptor binding — produces cardioprotective effects in ischemia models independently of GH release
- Dual research utility: GHS-R1a agonism for GH research + CD36-mediated cardiac biology research
- Reference maximum-potency GHRP for dose-response studies examining GHS-R1a activation ceiling
- Enables mechanistic dissection: GHS-R1a antagonism vs CD36 blockade to attribute observed cardiac effects
Research audience
Who researches Hexarelin Acetate?
Hexarelin is used by researchers in GHS-R1a pharmacology, GH secretagogue potency characterization, cardiac ischemia biology, CD36 receptor pharmacology, and dual-mechanism research requiring the highest-potency GHRP alongside a non-GH cardiac receptor dimension.
Preclinical research overview
What does the preclinical literature say about Hexarelin Acetate?
Hexarelin's development history tracks alongside the broader GHRP class: discovered in the context of systematically modifying GHRP-6 for increased potency, taken through animal pharmacology and into human Phase II research, then discontinued before approval as the GH secretagogue field consolidated around different therapeutic approaches. The Phase II dataset remains in the published literature and constitutes the most rigorous human pharmacokinetic characterization available for a GHRP-class compound outside Japan (where GHRP-2/Pralmorelin is approved).
The CD36 discovery was significant: it identified that hexarelin's cardioprotective effects in ischemia models were not abolished by GH receptor antagonism — ruling out an IGF-1-mediated cardioprotection pathway and implicating CD36 directly. Subsequent studies in CD36-null mice confirmed that the cardioprotective effects were CD36-dependent, establishing this receptor as a pharmacological target for peptide-based cardiac intervention research.
This cardiac biology dimension has made hexarelin relevant to a different research community than standard GHRPs — cardiovascular researchers studying ischemic preconditioning, cardiac repair, and scavenger receptor biology have incorporated hexarelin as a pharmacological probe for CD36's role in cardiomyocyte survival and stress response.
Common questions
Frequently asked about Hexarelin Acetate
Why use hexarelin over ipamorelin for GH research?
Ipamorelin is the preferred selective GHRP when isolated GH effects without cortisol or prolactin co-stimulation are needed. Hexarelin is preferred when: (1) maximum GH response is needed regardless of cortisol/prolactin confounders; (2) the research includes cardiac endpoints where CD36-mediated effects are relevant; (3) potency comparison studies require the highest-potency GHRP as the reference point. These are complementary research tools rather than substitutes.
Is the CD36 cardiac research robust?
The CD36-mediated cardioprotection data from hexarelin studies spans multiple published preclinical studies across different ischemia model designs, and the CD36-dependence was confirmed using CD36-null mice in which hexarelin's cardioprotective effects were abolished. This constitutes a reasonably strong preclinical mechanistic evidence base. Human cardiac CD36 receptor pharmacology has not been directly studied with hexarelin in prospective clinical research.
What does hexarelin's non-selective receptor profile mean for cardiac research?
In cardiac research designs using hexarelin, both GHS-R1a and CD36 are engaged simultaneously. To attribute observed cardiac effects to CD36 specifically, researchers use GH receptor antagonists or conduct parallel experiments in GH receptor-deficient animal models. This mechanistic dissection approach is standard in hexarelin cardiac research and is documented across the published preclinical literature.
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