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Hexarelin 5 mg
Peptide Library · Profile
Hexarelin 5 mg
Hexarelin is the only compound in this class with a real cardiac literature in real patients — and that literature says the effect fades as the heart gets sicker. In healthy men one dose lifted ejection fraction from 64.0% to 70.7%. In eight patients with dilated cardiomyopathy at 16.7%, it did not move at all. That gradient is the opposite of how hexarelin is sold.
Ejection fraction, healthy men64 → 70.7%one IV dose · n = 7 · independent of growth hormone
Ejection fraction, dilated cardiomyopathyNo change16.7 → 17.7% · not significant · n = 8
Development statusDiscontinuedexamorelin · a real drug candidate, not a research chemical
On FDA's compounding listsNeitherunlike GHRP-2 and GHRP-6 — and that is not a clean bill
The short version
Plain English first. Everything below this section is the same material with the sources, the numbers and the caveats attached.
What it is
GHRP-6 plus a single methyl group — one small change, and a much stronger compound. It is also a genuine former drug candidate: it was given the international name examorelin, and its development was discontinued.
What has actually been measured
The only real cardiac data anyone in this class has in actual patients. In healthy men, a single dose lifted the heart’s ejection fraction from 64.0% to 70.7%. That effect is measured and it is real.
What has not been measured
Anything past about an hour. Every cardiac study is a single acute dose with roughly sixty minutes of follow-up and no clinical endpoint. Nobody has measured whether repeating it does anything, or whether the change in a number on an echocardiogram matters to anyone’s health.
What most people get wrong
The direction of the effect. It is assumed to help hearts that need help, but the effect fades as the heart gets sicker — in eight patients with dilated cardiomyopathy it did not move at all, even though growth hormone rose normally. The hormone response and the cardiac response come apart.
What Hexarelin is
A synthetic hexapeptide — GHRP-6 with a single methyl group added to its D-tryptophan. That one atom is the entire structural difference. We do not sell it; this is a reference entry.
| Sequence | His–D-2-Me-Trp–Ala–Trp–D-Phe–Lys–NH2 |
| Formula · free base | C47H58N12O6 |
| Molecular weight | 887.06 — our computation from the registered formula |
| CAS · UNII | 140703-51-1 · 09QF37C617 |
| INN | examorelin |
| Development codes | EP 23905 · MF 6003 |
The naming trap, and it is the single most common error made about this compound
Hexarelin's official name is examorelin. The anti-doping list uses that name and not “hexarelin.” The pharmaceutical development record files it under Examorelin too. A page that searches only for “hexarelin” concludes the compound is unregistered and undeveloped. It is neither.
What the salt costs
Like GHRP-6 and unlike GHRP-2, hexarelin has three basic sites — the N-terminal amine, the lysine side chain and the histidine imidazole — so a third counterion is chemically available. House arithmetic, on our listed 5 mg vial:
| Salt form | Counterion as % of mass | Free base in a labelled 5.00 mg |
|---|---|---|
| Free base | 0% | 5.000 mg |
| Mono-acetate | 6.34% | 4.683 mg |
| Mono-TFA | 11.39% | 4.430 mg |
| Di-TFA | 20.45% | 3.977 mg |
| Tri-TFA | 27.83% | 3.608 mg |
A vial labelled “5 mg” holds 3.61 to 5.00 mg of examorelin on salt form alone — a 27.8% spread, before purity, residual water or fill accuracy. Nothing on a typical research label resolves which.
It was a real drug candidate
This is the fact that reframes everything else on the page, and almost nobody selling hexarelin mentions it.
Hexarelin was not born as a research chemical. It has an INN, two company development codes, a named originator — Mediolanum Farmaceutici, Milan — and a named indication, growth hormone deficiency.
Its highest development status, from the pharmaceutical development record: “Discontinued.”
What we can say, and it is well supported. Hexarelin was a pharmaceutical company's development compound and that development was stopped. We found no evidence it was approved in any jurisdiction — three differently-phrased searches, all named in our references note. The trials it did run are the ones set out below: small, acute, academic, and mostly from one group in Turin.
And what must not be written, including by us
That it “failed phase III.” We do not know that it reached phase III. The record's phase, its discontinuation date, and any stated reason all sit behind a subscription wall we could not pass.
Or any reason for the discontinuation. The obvious candidates are sitting right there on this page — sixteen-week desensitisation, flat IGF-1, no cardiac effect in the sickest hearts — and every one of them is our inference from the published pharmacology, not a documented account. They are worth noticing. They are not an explanation, and we are not going to dress them up as one.
Set that against GHRP-2, whose Japanese approval we document from the licensed label itself. Two compounds, one methyl group and one sequence swap apart: one became a licensed medicine for a one-hour diagnostic test, the other was developed as a therapeutic and abandoned. Both are now sold in vials to the public.
The cardiac literature
Four human studies. All acute, all intravenous, all at 2.0 µg/kg where a dose is stated. This is the most distinctive material about hexarelin and it is genuinely interesting — which is why it deserves to be read properly rather than quoted in half.
| Population | n | Baseline LVEF | After hexarelin |
|---|---|---|---|
| Healthy men | 7 | 64.0% | 70.7% — p < 0.03 |
| Growth-hormone-deficient adults | 7 | 50.0% | increased — p < 0.05 |
| Ischaemic cardiomyopathy | 5 | 22.6% | 26.2% — p < 0.05 |
| Dilated cardiomyopathy | 8 | 16.7% | 17.7% — not significant |
The gradient is the finding
House arithmetic from the figures above: the inotropic effect is largest in the hearts that need it least and vanishes in the hearts that need it most. In the dilated-cardiomyopathy patients growth hormone rose normally and the ejection fraction did not move — so it is not that the drug failed to reach them. That is the single most important sentence available about hexarelin and the heart, and it is the opposite of how hexarelin is marketed.
The strongest study, and the one thing it settles
The exception to “small and academic” is a study of 24 men with coronary artery disease during bypass surgery — four arms: hexarelin, GHRH, recombinant human growth hormone, and placebo.
Hexarelin alone improved ejection fraction, cardiac index and cardiac output (all p < 0.001, lasting to 90 minutes) and lowered wedge pressure (p < 0.01), “without any relevant variation in systemic vascular resistance.” The other three arms showed no effect.
Recombinant growth hormone itself did nothing. That is what turns “growth-hormone-independent” from an inference into a result — and it is the only study here with a placebo arm and active comparators. We have the significance levels but not the magnitudes, and we are not going to invent them.
Now the denominator, which no source states
Our reading of the published cohorts, labelled as such. Read the four studies together and a structural fact appears: this is not four independent studies. The healthy group is the same seven men, with the same 64.0% baseline, in two of them. The growth-hormone-deficient group is the same seven in two of them. The cardiomyopathy patients described as “12 with severe dilated cardiomyopathy” in one paper are plainly the same clinical series later split into 8 dilated and 5 ischaemic. The author lists overlap almost completely.
So the entire published human hexarelin cardiac literature is roughly thirty to forty patients, several of them counted more than once — plus the separate 24-patient bypass study. That is the honest denominator, and stating it does not make the finding go away. It makes it the right size.
Further caveats, because the finding is small in every direction. Five patients in the positive ischaemic group. Eight in the negative dilated group. A single acute intravenous dose. Sixty minutes of follow-up. And no clinical endpoint of any kind — no symptoms, no exercise capacity, no hospitalisation, no mortality. “Improves ejection fraction” here is a sixty-minute echocardiographic observation, not a treatment effect.
A fifth study we could not open
A paper on hexarelin in hypopituitary adults exists and would not open for us. A review describes it as reporting increased ejection fraction in seven growth-hormone-deficient patients with left ventricular failure. That is a review's sentence, not our reading of the paper, and we cannot tell whether its seven patients are a fourth cohort or the same seven counted again — which bears directly on the denominator above.
The rest of the evidence
Outside the heart, hexarelin's record is the class record, and it is not flattering.
It desensitises — and then recovers, which is a point in its favour
The longest exposure study in this entire class is hexarelin's: 1.5 µg/kg subcutaneously twice daily for sixteen weeks.
| GH response, week 0 | 19.1 µg/L·h |
| GH response, week 16 | 10.5 — house arithmetic: −45.0% |
| GH response, week 20 (four weeks off) | 19.4 — 101.6% of baseline |
| IGF-1 and IGFBP-3 across 20 weeks | No significant change |
The authors' own words: “a partial and reversible attenuation of the GH response,” and that “the biological impact of this hexarelin schedule on the GH-IGF-I axis seems to be minimal.”
Reversible is the operative word and it belongs here as a point in the compound's favour. The response comes back. But read the second quotation as carefully as the first: sixteen weeks of twice-daily injections, and the axis the whole class is named after barely moved.
The three desensitisation rates
A separate 24-hour study found that prior repeated dosing “blunted the GH response, abolished that of ACTH and cortisol and did not modify the PRL increase.”
Our reading, flagged as ours, of one six-person study: the corticotroph desensitises fastest, the somatotroph partially, and the lactotroph not at all — the effect you want fades, the cortisol effect fades, and prolactin is the one that stays. If that generalises it is the sharpest available statement about this class's side effects. It is currently one small study.
Cortisol and prolactin, with the number that surprises people
The dose-response study for hexarelin found a growth hormone ED50 of 0.48 µg/kg and a prolactin ED50 of 0.39 µg/kg.
House arithmetic: the prolactin curve sits below the growth hormone curve. That destroys the standard harm-reduction advice — “use a low enough dose to get GH without prolactin.” On these data there is no dose window that spares prolactin, and if anything the reverse. Cortisol behaves differently, stepping to about 40% at 0.5 µg/kg, more like a threshold.
And the combination argument, which is real: hexarelin plus a GHRH fragment reached 82% of maximal GH release on one-eighth the hexarelin dose, with “no rise in serum cortisol.” Concede that first. Then the correction from the same sentence of the same paper: it did not abolish the prolactin rise — still up 84.9%. Cortisol yes, prolactin no.
Appetite — the silence is a gap, not a difference
Hexarelin has no appetite reputation, and that is easy to read as “the GHRP without the hunger.” It is not that. Nobody has asked the question in humans.
What exists is a rat study: 80–320 µg/kg, with 80 µg/kg daily for eight weeks producing “a persistent significant orexigenic action throughout the treatment period” in both young and old animals.
So hexarelin is orexigenic in rats, persistently, over eight weeks. The absence of a hexarelin hunger claim in the marketplace is an artefact of nobody having measured it in a person, not evidence that it does not stimulate appetite.
And one more line from that study worth carrying: eight weeks of persistent appetite stimulation produced no weight gain. A rodent result that does not transfer — but a useful corrective to the assumption that appetite is the mechanism by which any of these compounds would change body composition.
No pharmacokinetics at all
We found no pharmacokinetic study of hexarelin. None. So no half-life appears on this page, and any figure you see quoted elsewhere is unsourced. The published pharmacokinetics on the GHRP-2 page belong to pralmorelin and do not transfer to a different molecule.
And the one sleep study, which we could not open
A 2004 paper exists whose title says hexarelin decreases slow-wave sleep while stimulating growth hormone, ACTH, cortisol and prolactin overnight. We could not open it and will not characterise its findings. Flagging it because if it says what its title says, then set against GHRP-6 — which increased only the light stage and left deep sleep untouched — the “GHRPs improve sleep” line would be contradicted by both compounds' own sleep studies.
Reconstitution
One genuine advantage of the smaller vial, and it is arithmetic.
House arithmetic. 5 mg vial, U-100 syringe, 1 unit = 0.01 mL.
| Diluent | Concentration | µg per unit | 100 µg | 200 µg | Half a unit, as % of a 100 µg dose |
|---|---|---|---|---|---|
| 1 mL | 5,000 µg/mL | 50 µg | 2 u | 4 u | ±25% |
| 2 mL | 2,500 µg/mL | 25 µg | 4 u | 8 u | ±12.5% |
| 3 mL | 1,667 µg/mL | 16.7 µg | 6 u | 12 u | ±8.3% |
| 5 mL | 1,000 µg/mL | 10 µg | 10 u | 20 u | ±5% |
The smaller vial is the more measurable one. At any given diluent volume a 5 mg vial is exactly half the concentration of a 10 mg vial, so every dose is twice as many syringe units and the read error halves. That is the opposite of the intuition that a bigger vial is better value — on a microgram-scale compound, concentration is the enemy of accuracy.
For scale, the studies on this page used 2.0 µg/kg intravenously — 160 µg at 80 kg, which is 6.4 units from this vial in 2 mL. The sixteen-week study used 1.5 µg/kg subcutaneously twice daily: 120 µg, or 4.8 units, twice a day. Those are study doses given in clinical settings, not a protocol, and two of them land on a fraction of a unit a U-100 barrel cannot resolve.
Under our 28-day in-use convention, a 5 mg vial at 100 µg/day delivers 2.8 mg and discards 2.2 mg — 44% of the vial. House arithmetic.
Storage
Lyophilised: cool, sealed, dark, desiccated. Reconstituted: 2–8 °C, in the dark, under our 28-day convention — which we publish as “a handling convention that has become repeated as though it were data.”
We found no published stability study of reconstituted hexarelin in any diluent at any temperature. The only regulator-approved handling statement in this class belongs to the licensed pralmorelin product, and it is a different molecule in a different formulation by a different route — it neither supports nor contradicts our 28 days.
Regulatory status
Here the headline inverts from the other two pages in this family, and the inversion is not good news.
Hexarelin is on neither FDA compounding table
We re-read the live page and searched it under both names. Neither “hexarelin” nor “examorelin” appears anywhere on it — not in Category 2, and not on the separate “nominated but withdrawn” list. GHRP-2 and GHRP-6 are both in Category 2. Hexarelin is not.
That is not a clean bill of health, and reading it as one is the error to avoid. Absence from the page means FDA has not assessed the substance in this programme. For a compound that was once a named pharmaceutical development candidate, that is a statement about attention, not about safety.
Canada
Hexarelin is named on Health Canada's 1 August 2025 seizure advisory, alongside GHRP-2 and GHRP-6. It is not named on the 9 April 2026 research-use-only advisory — we checked both directly rather than assuming either. It is named on the College of Physicians & Surgeons of Alberta notice of the same date, which is our own province.
And the general rule reaches it either way: “In Canada, peptides are generally regulated as prescription drugs,” and research-use-only labelling “does not make these products legal or exempt from regulatory requirements.”
Sport — and the name it hides under
Prohibited at all times, in and out of competition, in the growth-hormone-releasing peptides group — listed only as “examorelin.” The word “hexarelin” does not appear on the list at all.
Which is exactly why the naming trap at the top of this page matters. An athlete searching the prohibited list for “hexarelin” finds nothing and could reasonably conclude it is permitted. It is not. And everything in that class is a non-Specified substance, which attracts the standard sanction and puts a heavier burden on the athlete to reduce it.
Sentient Biogenix does not sell hexarelin.
Questions we actually get
Is hexarelin the one that's good for the heart?
It is the only one in this class with human cardiac data in patients, which is genuinely distinctive. But read the gradient: the effect was largest in healthy hearts, smaller in ischaemic cardiomyopathy, and absent in dilated cardiomyopathy — where growth hormone still rose, so the drug was reaching them. It is a sixty-minute observation, not a treatment effect.
How many patients is that based on?
Fewer than it looks. Our reading of the cohorts is that the whole published human cardiac literature is roughly thirty to forty patients, several counted more than once across overlapping papers from one group — plus a separate 24-patient bypass study, which is the strongest of them.
Was hexarelin ever a real drug?
Yes. INN examorelin, two development codes, a named originator, and growth hormone deficiency as the indication. Development status: discontinued. We could not find that it was ever approved anywhere, and we could not find out what phase it reached or why it stopped.
How is it different from GHRP-6?
By one methyl group on one residue. Everything else about the molecule is identical. What differs is the evidence: GHRP-6 has the endocrine studies and the FDA listing; hexarelin has the cardiac studies and a development history.
Does it cause less prolactin than the others?
Not that anyone has shown. The ranking everyone repeats traces to vendor pages, not to a head-to-head study. And hexarelin's own dose-response data show the prolactin curve sitting below the growth hormone curve — so there is no low-dose window that spares it.
Will it make me hungry?
Probably, and nobody has checked. It is persistently orexigenic in rats over eight weeks. There is no human appetite study. “The GHRP without the hunger” asserts something for which we found no evidence in either direction.
What's the half-life?
Unknown. We found no pharmacokinetic study of hexarelin at all — not one that we could not open, one that does not appear to exist. Any figure quoted elsewhere is unsourced.
It's not on FDA's do-not-compound list. Is that good?
No, it is just quiet. GHRP-2 and GHRP-6 are both on Category 2; hexarelin is on neither table. That means FDA has not looked at it in that programme — a statement about attention, not about safety.
References
- Bisi G, Podio V, Valetto MR, Broglio F, et al. Acute cardiovascular and hormonal effects of GH and hexarelin, a synthetic GH-releasing peptide, in humans. Journal of Endocrinological Investigation 1999;22(4):266–272. DOI 10.1007/BF03343555 — the healthy-men LVEF finding.
- Broglio F, Benso A, Valetto MR, et al. Growth hormone-independent cardiotropic activities of growth hormone-releasing peptides in normal subjects, in patients with growth hormone deficiency, and in patients with idiopathic or ischemic dilated cardiomyopathy. Endocrine 2001;14(1):105–108. DOI 10.1385/ENDO:14:1:105 — the three groups at once, and the first sign of the ceiling.
- Imazio M, Bobbio M, Broglio F, et al. GH-independent cardiotropic activities of hexarelin in patients with severe left ventricular dysfunction due to dilated and ischemic cardiomyopathy. European Journal of Heart Failure 2002;4(2):185–191. DOI 10.1016/s1388-9842(01)00223-9. PMID 11959048 — the split by aetiology, and the negative result in dilated cardiomyopathy. Read via the University of Turin repository record.
- Broglio F, Guarracino F, Benso A, et al. Effects of acute hexarelin administration on cardiac performance in patients with coronary artery disease during by-pass surgery. European Journal of Pharmacology 2002;448(2–3):193–200 — the strongest study: placebo-controlled, with recombinant GH and GHRH as active comparators, and recombinant GH did nothing. Significance levels only; the magnitudes are not in the abstract.
- Rahim A, O'Neill PA, Shalet SM. Growth hormone status during long-term hexarelin therapy. Journal of Clinical Endocrinology and Metabolism 1998;83(5):1644–1649 — sixteen weeks, 45% attenuation, full recovery by week 20, IGF-1 flat throughout. Abstract only; the sample size is not in it, which is why no n appears above.
- Massoud AF, Hindmarsh PC, Brook CG. Hexarelin-induced growth hormone, cortisol, and prolactin release: a dose-response study. Journal of Clinical Endocrinology and Metabolism 1996;81(12):4338–41 — the ED50 figures and the combination result.
- Maccario M, Veldhuis JD, Broglio F, et al. Impact of two or three daily subcutaneous injections of hexarelin on 24-h GH, prolactin, adrenocorticotropin and cortisol secretion in humans. European Journal of Endocrinology 2002;146(3):310–318 — the three desensitisation rates.
- Bresciani E, Pitsikas N, Tamiazzo L, et al. Feeding behavior during long-term hexarelin administration in young and old rats. Journal of Endocrinological Investigation 2008;31(7):647–652 — eight weeks of persistent orexigenic action, and no weight gain.
- AdisInsight drug record 800003697, filed under Examorelin — development codes EP 23905 and MF 6003, originator Mediolanum, highest status “Discontinued” for somatotropin deficiency. Phase, date and reason are behind a subscription wall we could not pass.
- US Food and Drug Administration. Certain bulk drug substances for use in compounding that may present significant safety risks — content current 22 April 2026. fda.gov — read directly and searched under both names. Hexarelin and examorelin appear on neither table.
- Health Canada. Unauthorized injectable peptide drugs seized and sold by Canada Peptide, 1 August 2025 — hexarelin named. And: Think twice before injecting peptides bought online, 9 April 2026 — not named, checked by direct read. College of Physicians & Surgeons of Alberta, 9 April 2026 — named.
- The 2026 Prohibited List, World Anti-Doping Code — examorelin, growth hormone releasing peptides group. Read through a national anti-doping organisation's verbatim reproduction.
What we could not check, listed rather than hidden. The most important gap is why development stopped and what phase it reached — the review most likely to settle both returned a publisher block on three attempts, and the development record's own answer is behind a subscription wall. We found no pharmacokinetic study of hexarelin at all, so this page prints no half-life. We could not open the hypopituitary-adults cardiac paper, which bears on whether its seven patients are a fourth cohort or the same seven counted again; the 2004 sleep paper, whose title points somewhere interesting; the sixteen-week study's full text, which is why no sample size appears for it; or the two primary papers on CD36, the second receptor. Three named searches found no evidence of approval in any jurisdiction — a negative with the queries behind it, not a proof. And the cohort-overlap reading in the cardiac section is ours: no source states that denominator.
For laboratory research use only. Not for human or veterinary use. Nothing on this page is dosing guidance, and no figure here should be read as a recommendation.