HEALING & REPAIRPreclinicalTELOMERASEANTI-AGINGLONGEVITY

Epithalon

Also known as: Epitalon · Epithalone · Ala-Glu-Asp-Gly

19.9k views/week 312 citations 0 edits Updated 5/24/2026

Epithalon is a synthetic tetrapeptide analog of Epithalamin — a polypeptide extract of the pineal gland — developed by Professor Vladimir Khavinson at the St. Petersburg Institute of Bioregulation. It is notable for activating telomerase, the enzyme responsible for telomere elongation, with potential longevity applications.

STRUCTURE

Molecular Composition

FORMULA
C₁₄H₂₂N₄O₄
MOL. WEIGHT
310.35 Da
SEQUENCE LENGTH
4 amino acids
CAS NUMBER
307297-39-8
ORIGIN
Epithalamin extract
SOLUBILITY
Water-soluble
AMINO ACID CHAIN VISUALIZATION
E
Glutamate
N-terminal start
NH-CO
A
Alanine
spacer
NH-CO
G
Glycine
flexible linker
NH-CO
L
Leucine
C-terminal cap
SEQUENCEE-A-G-L
MECHANISMS

How It Works

🧬
Telomerase Activation
Epithalon upregulates telomerase (TERT) expression in human cells, enabling telomere lengthening and restoration of telomere-associated DNA damage foci. This mechanism directly counters the progressive telomere shortening associated with cellular aging and replicative senescence.
🌙
Pineal Gland Regulation
As a derivative of epithalamin (the pineal gland's primary peptide), Epithalon restores pinealocyte function and melatonin production. This addresses the age-related calcification and functional decline of the pineal gland that contributes to sleep disruption and circadian rhythm disorders.
🛡
Antioxidant & DNA Protection
Epithalon reduces oxidative stress in nuclear DNA and enhances DNA repair enzyme activity. Studies show decreased 8-oxoguanine levels and improved DNA integrity in treated cells — mechanisms that complement telomerase activation for comprehensive anti-aging effects.
Melatonin Pathway Enhancement
Beyond direct telomerase effects, Epithalon modulates the melatonin signaling pathway, improving sleep architecture and circadian rhythm synchronization. This creates a feedback loop where improved sleep further supports pineal gland function and telomere maintenance.
OVERVIEW

Research Overview

Epithalon was developed in Russia over several decades of research on pineal gland bioregulators. The peptide is a synthetic version of the natural tetrapeptide produced by the pineal gland epithelium, and has been studied extensively in both animal models and human trials — some spanning 15+ years — making it one of the most longitudinally studied peptide bioregulators.

Its primary claim to scientific attention is the activation of telomerase reverse transcriptase (TERT), the catalytic subunit of the telomerase complex. By elongating telomeres — the protective caps on chromosomal DNA that shorten with each cell division — Epithalon may delay cellular senescence and extend healthy cell lifespan. Human trials by Khavinson et al. showed 12–16% reductions in mortality in elderly cohorts.

Mechanism of Action

// TELOMERASE ACTIVATION

Epithalon upregulates expression of hTERT (human telomerase reverse transcriptase), the catalytic core of telomerase. This enables somatic cells — which normally lack active telomerase — to elongate shortened telomeres, reversing a key hallmark of cellular aging and reducing replicative senescence.

// PINEAL-MELATONIN AXIS RESTORATION

Epithalon restores age-related decline in pineal gland melatonin secretion by normalizing the activity of hydroxyindole-O-methyltransferase (HIOMT), the enzyme responsible for melatonin synthesis. Restored melatonin levels improve circadian rhythm regulation and antioxidant defense.

// ANTIOXIDANT & DNA REPAIR

Epithalon upregulates superoxide dismutase (SOD) and catalase expression, reducing oxidative stress. It also enhances DNA mismatch repair pathways, reducing mutation accumulation in aging tissues.

DOSAGE

Dosage & Administration

INJECTABLE (SUBCUTANEOUS)
DOSE
100–500 µg
FREQUENCY
Once daily at bedtime
NOTES
Most common route. Administer subcutaneously in the evening when natural melatonin levels are rising. Reconstitute with bacteriostatic water. Store refrigerated after reconstitution.
ORAL (SUBLINGUAL)
DOSE
500–1000 µg
FREQUENCY
Once daily at bedtime
NOTES
Sublingual administration may provide better bioavailability than swallowed oral doses. Hold under tongue for 5–10 minutes before swallowing. Less studied than injectable route.
INTRANASAL
DOSE
200–400 µg
FREQUENCY
Once daily at bedtime
NOTES
Direct CNS delivery via olfactory pathway. Lower systemic exposure than injectable but potentially better brain penetration. Experimental route with limited data.

Epithalon (Epitalon) is a synthetic tetrapeptide derived from the natural pineal gland peptide epithalamin. It has been extensively studied in Russian research for over 30 years, with particular focus on telomere biology and aging. No significant adverse effects reported in research protocols. The peptide is stable and does not require special storage conditions when lyophilized.

CYCLING

Cycle Duration Guide

ON CYCLE
3–6 months (long-term use common in anti-aging protocols)
OFF CYCLE
1–2 months

Epithalon is often used in extended cycles due to its cumulative effects on telomere length and pineal gland function. Many researchers run continuous 6-month courses with periodic breaks. Effects on sleep quality and melatonin production typically appear within 2–4 weeks, while telomere effects may take 3–6 months to become measurable.

Quick Reference
FORMULAC₁₄H₂₂N₄O₉
MOL. WEIGHT390.35 Da
LENGTH4 amino acids
ORIGINSynthetic analog of pineal gland tetrapeptide Epithalamin; developed in Russia
HALF-LIFE~30 minutes plasma; subcutaneous or intranasal administration
SOLUBILITYSoluble in bacteriostatic water or saline
CAS NO.307297-39-8
STATUSPreclinical
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TAGS
telomeraseanti-aginglongevitypineal glandmelatoninDNA repair