N-Acetyl Epithalon Amidate

N-Acetyl Epithalon Amidate is a research-chemical variant of Epitalon (Ala-Glu-Asp-Gly), the four-amino-acid pineal peptide synthesized by Vladimir Khavinson's group in St.

Educational summaryPeptide research profile

Dosing & scaling, explained

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Evidence context

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Storage, handling and interpretation

Product identity

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Reported protocols for N-Acetyl Epithalon Amidate

What published studies and recent community write-ups report about amounts, timing and course length. 2 clinical, 4 preclinical and 5 community-reported rows, each linked to its source. These are descriptions of what others report, not instructions, and nothing here is medical advice.

ContextDoseFrequencyRouteCourseSource
Clinical2 rows
Retinitis pigmentosa series at the originating institute (parent Epitalon)162 patients with retinitis pigmentosa aged 18-72, compared with conventionally treated controls5 mcg per eyeOnce dailyParabulbar injection10 consecutive daysNot describedInternational Journal of Molecular Sciences (PubMed Central)2025
As summarized in a 2025 independent review, visual acuity rose by 0.15-0.20 on average, visual field borders widened in all treated patients (by 90-120 degrees in 64.8%) and no side effects were reported; the original 2002 paper claimed a positive effect in 90% of cases. The study was open-label and unblinded, the control group received unrelated vasoactive drugs, and the dose is roughly a thousandth of the milligram amounts sold for systemic use.
Sublingual circadian study in women (parent Epitalon)75 women, with placebo and untreated control groups0.5 mg per dayOnce dailySublingual20 daysNot describedInternational Journal of Molecular Sciences (PubMed Central)2025
Urinary 6-sulfatoxymelatonin, a marker of pineal melatonin output, was 1.6 times higher than in the placebo group, Clock gene expression in leukocytes fell 1.8-fold and Cry2 expression doubled. The review that reports these figures notes that the human Epitalon literature consists of such small, single-center studies from the developer's institute without modern randomized designs.
Preclinical4 rows
Lifelong rodent geroprotection study (parent Epitalon)108 female Swiss-derived SHR mice, 54 per group, dosed from age 3 months until natural death1 mcg per mouse (roughly 30-40 mcg/kg) in 0.1 mL salineOnce daily on 5 consecutive days each monthSubcutaneousLifelong monthly coursesAbout 25 days off between each 5-day courseBiogerontology (PubMed)2003
Mean lifespan did not change, but the last 10% of survivors lived 13.3% longer, maximum lifespan rose 12.3%, bone-marrow chromosome aberrations fell 17.1% and leukemia incidence dropped 6-fold. Total spontaneous tumor incidence was unchanged, and the authors read the result as evidence of long-term safety in mice rather than as a human dosing guide.
Transgenic breast cancer mouse model (parent Epitalon)Female FVB/N HER-2/neu transgenic mice, treated from age 2 months1 mcg per mouseOnce daily on 5 consecutive days each monthSubcutaneousMonthly courses for lifeRemainder of each month offInternational Journal of Cancer (PubMed)2002
Epitalon reduced the cumulative number and maximum size of mammary tumors and the size of lung metastases, with a 3.7-fold drop in HER-2/neu mRNA in tumors. The dipeptide Vilon given on the same schedule worsened tumor outcomes, which shows that short peptides from this program are not interchangeable.
Low-dose spontaneous carcinogenesis study (parent Epitalon)One-year-old female C3H/He mice followed for 6.5 months0.1 mcg per mouse5 times a weekInjection (route not specified in the abstract)6.5 monthsWeekends offIn Vivo (PubMed)2006
This Israeli group, working with Anisimov, used a dose ten times lower than the St. Petersburg studies and saw no toxicity, fewer mice with malignant tumors and no metastases versus 3 of 9 tumor-bearing controls. It is one of the few Epitalon animal studies with authors outside the originating institute.
Independent in vitro telomere study (parent Epitalon)Human breast cancer lines (21NT, BT474) and normal fibroblast (IBR.3) and epithelial (HMEC) cells0.1, 0.2, 0.5 or 1.0 mcg/mL in culture mediumFresh peptide added dailyCell culture (stock made by dissolving 10 mg in 4 mL bacteriostatic water)4 days for cancer cells; 3 weeks for normal cellsNot applicableBiogerontology (PubMed Central)2025
A Brunel University group confirmed telomere lengthening outside the Khavinson lineage: normal cells needed three weeks at 1 mcg/mL and lengthened telomeres through hTERT and telomerase induction, while cancer lines lengthened telomeres within four days through ALT activity instead. BT474 cells peaked at 0.2 mcg/mL with smaller effects at higher concentrations, a non-linear pattern that complicates any dose extrapolation.

How a course is commonly described

  1. Days 1-10 (or 1-20)Community-reported

    Community courses run the full dose from day one, 10 mg nightly for 10 days or 5 mg nightly for 20 days, injected subcutaneously at a consistent evening time. Early user reports are of sleep changes and vivid dreams within days; no measurable endpoint is expected during the course itself.

  2. Analog-specific adjustmentsCommunity-reported

    Guides written for the acetylated amidated form copy the same 10-20 day course but some drop the dose to 1-3 mg on the assumption that the caps slow breakdown. Both 2026 guides that cover the analog stress that this assumption is untested and that no pharmacokinetic study of the capped molecule exists.

  3. Months 1-6: breakCommunity-reported

    Every community source describes months off after a course, typically 4-6 months, giving 1-3 courses a year. The rationale offered is that the Russian follow-up cohorts received spaced Epithalamin courses (six over three years in one study) and that effects were said to persist between them.

  4. Clinical comparisonClinical

    The published human Epitalon studies used 5 mcg per eye for 10 days or 0.5 mg sublingually for 20 days, far below the 5-10 mg daily injections described online. The mortality and cardiovascular findings that community guides cite come from courses of the Epithalamin extract in Russian and Ukrainian cohorts, a different preparation given to 266 people over 60 and followed for 6-8 years.

  5. Dose-translation caveatPreclinical

    A 2026 translational analysis argues that the 5-10 mg convention was carried over from Epithalamin, which needed about 500 times more material than Epitalon to produce the same melatonin response in old monkeys, and that scaling the effective 1 mcg per mouse dose to a 70 kg adult gives roughly 190-230 mcg per treatment day. It proposes formal dose-finding in the 100-300 mcg range rather than endorsing either figure.

  • No study of any kind has been published on the acetylated amidated form itself. Every protocol above either tests the parent tetrapeptide Epitalon or copies its vendor conventions, and the claimed longer half-life of the capped peptide is a chemistry inference rather than a measured value.
  • The human evidence for the parent compound is thin: small open-label series from the developer's institute, mostly using microgram eye injections or a 0.5 mg sublingual dose. The 5-10 mg daily course sold online matches neither, and one 2026 analysis suggests it may be one to two orders of magnitude above an allometrically scaled dose.
  • Neither Epitalon nor the analog is approved by any regulator or listed for pharmacy compounding, and the telomerase mechanism raises an unresolved theoretical cancer question that the animal tumor data do not settle. The rows above record what sources report, not endorsements of use.
Sources for this section (12)
  1. Overview of Epitalon-Highly Bioactive Pineal Tetrapeptide with Promising PropertiesInternational Journal of Molecular Sciences (PubMed Central)2025Clinical
  2. Peptides of pineal gland and thymus prolong human lifeNeuro Endocrinology Letters (PubMed)2003Clinical
  3. Effect of Epitalon on biomarkers of aging, life span and spontaneous tumor incidence in female Swiss-derived SHR miceBiogerontology (PubMed)2003Preclinical
  4. Inhibitory effect of the peptide epitalon on the development of spontaneous mammary tumors in HER-2/neu transgenic miceInternational Journal of Cancer (PubMed)2002Preclinical
  5. Effect of the synthetic pineal peptide epitalon on spontaneous carcinogenesis in female C3H/He miceIn Vivo (PubMed)2006Preclinical
  6. Epitalon increases telomere length in human cell lines through telomerase upregulation or ALT activityBiogerontology (PubMed Central)2025Preclinical
  7. The microgram hypothesis: a translational dosing error in Epitalon peptide research and its implications for human aging applicationAging Pathobiology and Therapeutics2026Preclinical

Plus 5 community resources (dosing guides, forum threads and vendor write-ups), reported above but not linked.

Overview

N-Acetyl Epithalon Amidate is a research-chemical variant of Epitalon (Ala-Glu-Asp-Gly), the four-amino-acid pineal peptide synthesized by Vladimir Khavinson's group in St. Petersburg from the amino acid composition of the bovine pineal extract Epithalamin. The acetyl cap on the N-terminus and the amide on the C-terminus are a standard chemistry strategy to slow breakdown by exopeptidases; no published pharmacokinetic or efficacy study has compared the capped form with the parent peptide in any species. Everything known about its biology therefore comes from Epitalon: cell-culture reports of telomerase induction, rodent studies of lifespan and tumor incidence, primate melatonin work, and small open-label human series from the originating institute. Neither compound is approved by any regulator, and the analog is sold only as a lyophilized research vial.

What researchers are exploring

These themes organize the educational information currently available. Individual claims remain under source review and are not treatment claims.

  • 1

    What is N-Acetyl Epithalon Amidate?

    Introduction to the modified peptide and its research history

  • 2

    How does N-Acetyl Epithalon Amidate Work?

    Mechanisms of action and epigenetic modulation

  • 3

    Applications and Health Benefits

    Therapeutic potential across multiple systems

What is known and what still needs verification

Available context is organized without assigning unsupported study models or evidence grades.

  • Not graded

    What is N-Acetyl Epithalon Amidate?

    Introduction to the modified peptide and its research history

  • Not graded

    How does N-Acetyl Epithalon Amidate Work?

    Mechanisms of action and epigenetic modulation

Chemistry identifiers

Sequence, synonyms and registry identifiers as recorded in PubChem, the National Library of Medicine's open chemistry database. Formula, mass and CAS number are summarized at the top of the page.

Sequence

Ac-Ala-Glu-Asp-Gly-NH2

Also listed as

Epitalon, Epithalon, Epithalone, Ala-Glu-Asp-Gly, AEDG peptide, AE-0 peptide, UNII O65P17785G, CHEBI:230091

InChIKey

HGHOBRRUMWJWCU-FXQIFTODSA-N

IUPAC name

(4S)-4-[[(2S)-2-aminopropanoyl]amino]-5-[[(2S)-3-carboxy-1-(carboxymethylamino)-1-oxopropan-2-yl]amino]-5-oxopentanoic acid

Limitations and unknowns

Important limitations

  • Individual claims and source links have not yet completed editorial verification.
  • Evidence level, applicable study model, formulation, route and population remain unassigned.

Sources

1 link carried over from the earlier page, awaiting verification.

  1. Source link (pmc.ncbi.nlm.nih.gov)Verification pendingNot graded