Hexarelin
clinical trialsAlso known as: Examorelin, EP-23905
**Mechanism of Action** Hexarelin is a synthetic hexapeptide belonging to the growth hormone-releasing peptide (GHRP) family. It acts as a potent agonist at the ghrelin receptor (GHS-R1a), stimulating growth hormone (GH) secretion via the pituitary and hypothalamus. However, its cardioprotective effects are mediated through GH-independent pathways, including direct binding to CD36 (a scavenger receptor) on cardiomyocytes and endothelial cells, which activates anti-apoptotic signaling (e.g., PI3K/Akt) and reduces oxidative stress. This dual mechanism distinguishes Hexarelin from other GHRPs. **Key Research Findings** Clinical trials have demonstrated Hexarelin’s ability to improve cardiac function in patients with chronic heart failure, including increased left ventricular ejection fraction and reduced myocardial ischemia. Preclinical studies show it protects against doxorubicin-induced cardiotoxicity and ischemia-reperfusion injury by attenuating mitochondrial dysfunction and inflammation. Notably, its GH-releasing potency is approximately 10-fold greater than GHRP-6, with a longer half-life (~2 hours) due to resistance to enzymatic degradation. Adverse effects in trials include transient flushing and mild GH-related metabolic changes. **Clinical Relevance** Hexarelin is under investigation for acute and chronic cardiac conditions, particularly where GH-independent cardioprotection is desired. Its potential applications include adjunctive therapy in heart failure, post-myocardial infarction recovery, and prevention of chemotherapy-induced cardiotoxicity. However, its GH-releasing activity limits use in GH-sensitive malignancies. Further phase II/III trials are needed to establish safety and efficacy profiles. For research purposes only — not medical advice.
Key data
C47H58N12O6Research & studies
Hexarelin pretreatment reduced tubular necrosis, improved renal function, and inhibited apoptosis in I/R-induced AKI rats.; Hexarelin downregulated pro-apoptotic proteins (Caspase-3, Bax, Bad) and upregulated anti-apoptotic Bcl-2.; Molecular docking showed strong binding affinity between Hexarelin and MDM2, suggesting a mechanism via MDM2/p53 pathway.; Hexarelin suppressed MDM2 and p53 expression in both in vivo and in vitro experiments.
Hexarelin decreased infrarenal aorta diameter in elastase-induced AAA mice.; Hexarelin rescued smooth muscle cell contractile phenotype by increasing α-SMA and decreasing MMP2.; Hexarelin inhibited NLRP3 inflammasome activation, IL-18 production, and inflammatory cell infiltration.; Hexarelin suppressed NF-κB signaling pathway, a key initiator of inflammatory response.
GHRP (e.g., hexarelin) potently induces PPARγ through activation of the scavenger receptor CD36.; The CD36-PPARγ pathway regulates essential aspects of lipid and energy metabolism.; Activation of this pathway shows benefits on atherosclerosis, hepatic cholesterol biosynthesis, and fat mitochondrial biogenesis.; The PPARγ coactivator PGC-1 is involved in mediating these metabolic effects.
GHSs promote pulsatile GH release with negative feedback, reducing risk of supra-therapeutic GH levels.; Potential benefits include improved growth velocity in children, increased lean mass, and better sleep.; Available studies indicate GHSs are well tolerated, but may increase blood glucose due to decreased insulin sensitivity.; Long-term safety data, including cancer incidence and mortality, are lacking and require further research.
Frequently asked questions
What is Hexarelin?
**Mechanism of Action** Hexarelin is a synthetic hexapeptide belonging to the growth hormone-releasing peptide (GHRP) family. It acts as a potent agonist at the ghrelin receptor (GHS-R1a), stimulating growth hormone (GH) secretion via the pituitary and hypothalamus. However, its cardioprotective effects are mediated th
How does Hexarelin work?
Potent GHRP-family ghrelin receptor agonist with studied cardioprotective effects independent of GH release.
What is the research status of Hexarelin?
Hexarelin is currently classified as clinical trials, with 289 research references on record. This is for research purposes only and is not medical advice.
What is the molecular weight of Hexarelin?
Hexarelin has a molecular weight of approximately 887 g/mol (formula C47H58N12O6).
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