Hexarelin

The Hexarelin evidence base cited here is 8 sources — 2 clinical, 4 preclinical, 1 review. Its strongest evidence is human — 2 clinical studies, most recently 1994 ("Growth Hormone-Releasing Activity of Hexarelin in Humans: A Dose-Respons…"). Regulatory status: Not FDA-approved.

• Hexarelin (Examorelin) is a synthetic hexapeptide GH secretagogue — among the most POTENT GHRPs studied — derived from GHRP-6 with a single 2-methyl-Trp substitution for greater stability and potency.
• Beyond GH release (via the ghrelin/GHS-R1a receptor), it uniquely binds cardiac CD36 receptors, giving a GH-independent cardioprotective effect that's a distinct research interest.
• It reached Phase II human trials for GH deficiency and heart failure before being discontinued in 2005 for strategic (not safety) reasons — so it has more human data than most research peptides.

Hexarelin is a six-amino-acid growth-hormone-releasing peptide, developed by Mediolanum Farmaceutici as a more potent successor to GHRP-6. It stimulates GH release through the ghrelin receptor and, distinctively, acts on cardiac CD36 receptors for a heart-protective effect that doesn't depend on GH at all.

It is not FDA-approved; everything below is research context rather than medical guidance.

Hexarelin is a synthetic hexapeptide (~887 Da, sequence His-D-2-methyl-Trp-Ala-Trp-D-Phe-Lys-NH₂). It is structurally near-identical to GHRP-6 — the one change is a 2-methyl-tryptophan substitution at position 2, which improves proteolytic stability and boosts potency. It's a clean illustration of structure-activity tuning: a single residue swap turns GHRP-6 into the most potent GHRP in the class.

Hexarelin binds GHS-R1a on pituitary somatotrophs to trigger a pulse of GH release, peaking around 30 minutes and returning to baseline within a few hours. Separately, it activates cardiac CD36 receptors, producing anti-apoptotic and anti-fibrotic cardioprotective effects independent of growth hormone — the basis for its heart-failure research. As with other GHRPs, pairing it with a GHRH analog produces a markedly larger combined GH pulse.

There is no approved dosing. Figures below are research/anecdotal, included for research context only — and strict cycling matters more here than with gentler GHRPs.

• GH optimization: ~100 mcg subcutaneously, up to 3× per day (empty stomach — 2+ hours after eating, 30+ min before)
• Often combined: ~100 mcg hexarelin + ~100 mcg CJC-1295 for a larger pulse
• Cardioprotection research: ~100–200 mcg twice daily
• Strict cycling is essential: roughly 8–16 weeks on, then 4–6 weeks off — hexarelin desensitizes faster than ipamorelin

Hexarelin's GH response can fall ~40–50% by weeks 8–12; a 4–6 week break restores it to near-baseline. This faster desensitization is the trade-off for its higher potency.

• Reconstitute with bacteriostatic water added slowly down the vial wall; swirl/roll gently, never shake; solution should be clear and colorless.
• Refrigerate at 2–8°C and use within ~4 weeks; avoid pre-mixed solutions (degrade rapidly).
• Verify with a COA (>98% purity, correct ~887 Da mass); discard if discolored or cloudy.

Hexarelin is the most potent GHRP but also has the highest side-effect profile of the class. Unlike ipamorelin, it elevates cortisol and prolactin at standard doses (worth monitoring long-term, as prolactin elevation can contribute to secondary hypogonadism). It can cause water retention in the first 1–2 weeks and affect glucose metabolism (monitor if diabetic/pre-diabetic). Facial flushing after injection is common. It is not advisable with active cancer (GH/IGF-1 may promote tumor growth) and is WADA-prohibited. Partial desensitization is expected and reverses with cycling.

• GH-releasing activity in humans (1994): 0.5–2 µg/kg IV in adult males gave dose-dependent GH release peaking at 30 minutes (Cmax up to ~55 ng/mL vs ~3.9 placebo).
• Myocardial function after MI (2018, mouse): 0.3 mg/kg/day for 21 days after LAD ligation improved LV function and reduced LV collagen ~53%, with lower TNF-α/IL-1β.
• ALS neuroblastoma model (2023, in vitro): 1 µM protected SOD1-G93A cells against oxidative cytotoxicity (raised Bcl-2, reduced caspase-3, less DNA damage).

Hexarelin is not FDA-approved (its Phase II program was discontinued in 2005 for strategic reasons) and is sold as a research chemical for laboratory use only, not intended for human consumption. As a GH secretagogue it is prohibited in sport (WADA).

All citations link to the original source (PubMed, journal site, or regulatory filing). Independent research database — no vendor influence on what's cited.