Hexarelin

Description

What is Hexarelin?

Hexarelin (examorelin) is a synthetic hexapeptide, structurally related to GHRP‑6, developed in the 1990s as a potent oral / parenteral GH secretagogue. In addition to GH release, it has been studied for direct cardiac effects mediated through the CD36 receptor in cardiomyocytes.

Mechanism of Action

• Ghrelin‑receptor (GHS‑R1a) agonist – pulsatile GH release from pituitary
• Also binds the scavenger receptor CD36 in cardiac tissue, implicated in cardioprotective signaling in preclinical ischemia models
• Synergizes with GHRH for supra‑additive GH pulses
• Reported to induce some tachyphylaxis on repeated high‑dose administration (desensitization of GHS‑R1a)

Compound Properties

• Molecular formula: C₄₇H₅₈N₁₂O₆
• Molecular weight: ~887.04 g/mol
• CAS: 140703‑51‑1
• Sequence: His‑D‑2‑methyl‑Trp‑Ala‑Trp‑D‑Phe‑Lys‑NH₂
• Form: Lyophilized powder
• Unit size: 2 mg / vial (typical)
• Source: Solid‑phase peptide synthesis; ≥99% purity by HPLC

Research‑Reference Dosing

Published research‑reference ranges in clinical and preclinical literature:

• Imbimbo et al., European Journal of Clinical Pharmacology (1994): single‑dose PK/PD of IV and SC hexarelin in healthy males.
• Ghigo et al., JCEM (1994, 1996): GH‑releasing activity and interactions with GHRH in adults.
• Broglio et al., JCEM (2002): cardiovascular actions in healthy and cardiac‑patient cohorts.

Research Findings

• Among the most potent GHS peptides on molar basis (Ghigo 1994)
• Direct cardioprotective signaling via CD36 in rodent ischemia/reperfusion models
• Rapid desensitization reported with continuous high‑dose exposure

Known Side Effects Reported in Research/Trials

• Flushing, sweating, transient tachycardia
• Cortisol and prolactin elevation (class effect, more pronounced than ipamorelin)
• Possible desensitization of GH response with frequent dosing
• Injection‑site reactions

Storage & Handling

• Lyophilized (unreconstituted) vials: store at −20°C long‑term; short‑term 2–8°C acceptable.
• After reconstitution with bacteriostatic or sterile water: store at 2–8°C; use within 14–28 days per standard peptide stability guidance.
• Protect from light, heat, and repeated freeze‑thaw cycles. Handle in a sterile laboratory environment.

Certificate of Analysis

A Certificate of Analysis (COA) confirming identity and purity by HPLC / MS is available upon request. Contact Lonestar Peptides for lot‑specific documentation.

Summaries reference peer‑reviewed preclinical and clinical literature available as of early 2025. Newer findings may not be reflected. Researchers should consult current literature and conduct their own due diligence. Lonestar Peptides makes no claim of therapeutic benefit.