Hexarelin

Overview

Hexarelin (Examorelin) is a synthetic hexapeptide growth hormone secretagogue (GHS) that acts as a potent agonist at the GHS-R1a (ghrelin receptor). Developed in the 1990s, Hexarelin is one of the most potent GH-releasing peptides studied in clinical settings, producing greater GH release than GHRP-6, GHRP-2, or Ipamorelin. Uniquely, published research has identified cardioprotective effects of Hexarelin that are independent of GH release, mediated through a distinct cardiac receptor (CD36). This dual mechanism has made Hexarelin a particularly interesting research compound in both endocrine and cardiovascular research. Clinical studies have been conducted in healthy subjects, GH-deficient populations, and cardiac patients.

For research use only · Not FDA/EMA approved · Not for human consumption

Mechanism of Action

Hexarelin activates GHS-R1a receptors on pituitary somatotrophs through a mechanism similar to other GHS compounds but with higher potency. Published research describes a unique secondary mechanism: binding to CD36 (scavenger receptor class B, type 3) on cardiac myocytes. CD36-mediated signaling activates PPARγ (peroxisome proliferator-activated receptor gamma) and downstream anti-apoptotic pathways in cardiac tissue, providing GH-independent cardioprotection. Studies describe activation of ERK1/2 and Akt survival signaling in cardiomyocytes. Unlike Ipamorelin, Hexarelin causes some release of cortisol and prolactin at GH-stimulating doses, indicating less receptor selectivity.

For research use only · Not FDA/EMA approved · Not for human consumption

Key Research Areas

• Potent GH release and comparison with other GHS compounds
• CD36-mediated cardioprotection independent of GH axis
• Cardiac function improvement in Phase 2 heart failure trials
• Anti-apoptotic signaling in cardiomyocyte models
• GHS-R1a receptor pharmacology and structure-activity relationships
• PPARγ activation and metabolic effects in cardiac tissue

For research use only · Not FDA/EMA approved · Not for human consumption

Published Studies (6 cited)

For research use only · Not FDA/EMA approved · Not for human consumption

Dosage in Published Research

Published clinical studies have used Hexarelin at 1–2 μg/kg intravenously or 20 μg/kg subcutaneously in human studies. Cardiac studies used 20 μg/kg IV. Preclinical studies have employed 100–400 μg/kg in rodent models. Desensitization of GH response has been reported with continuous dosing. All dosing information is from published literature only.

For research use only · Not FDA/EMA approved · Not for human consumption

Storage & Handling

Store lyophilized Hexarelin at -20°C. Reconstituted solutions at 2–8°C, use within 14 days. The peptide is stable in solution at neutral pH. Handle with sterile laboratory technique.

For research use only · Not FDA/EMA approved · Not for human consumption

Safety Profile (Literature Only)

Published clinical studies report Hexarelin as generally well-tolerated. Unlike Ipamorelin, Hexarelin does cause some cortisol and prolactin release at GH-stimulating doses. Facial flushing and hunger sensation have been reported. Desensitization of GH response occurs with prolonged continuous use. No serious adverse events have been reported in published clinical studies at investigated doses. This compound is for laboratory research use only.

For research use only · Not FDA/EMA approved · Not for human consumption