Epithalon 50mg
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Compound Identity
COMPOUND NAME
Epithalon
SYNONYMS
Ala-Glu-Asp-Gly; epithalone; pineal peptide tetrapeptide
CAS NUMBER
307297-39-8
MOLECULAR FORMULA
C14H22N4O9
MOLECULAR WEIGHT
~390.35 g/mol
STRUCTURE
Synthetic tetrapeptide
PEPTIDE SEQUENCE
H-Ala-Glu-Asp-Gly-OH
CHEMICAL STRUCTURE

Molecular Formula: C14H22N4O9
Source: PubChem
Mechanism of Action
Epithalon functions by upregulating telomerase reverse tranceiptase (TERT) activity in somatic cells, which promotes telomere elongation and chromosomal stability. It also suppresses expression of certain oncogenes such as HER-2/neu, contributing to its antitumor effects. Additionally, Epithalon reduces oxidative stress and restores circadian melatonin secretion rhythms in aged animals2,3.
Activation of Telomerase Reverse Transcriptase (TERT)
Downregulation of HER-2/neu Expression
Biological Activity
Epithalon has been shown to increase lifespan in rodent models, reduce spontaneous and induced tumor formation, stabilize the genome by reducing chromosomal aberrations, and modulate immune cell proliferation. Its actions extend to radioprotective effects on the thymus and intestinal mucosa1,4.
Storage
- −20°C or below. Protect from light and moisture.
Drug Categories
Peptides; Bioregulators; Geroprotective Compounds
Additional Notes
- Originally synthesized at the St. Petersburg Institute of Bioregulation and Gerontology.
- Noted for unique pineal gland regulatory function and epigenetic modulation potential.
- Epithalon is a research-use-only compound. It is not FDA-approved and has not completed full clinical trials. It is supplied for laboratory investigation only and is not intended for diagnostic or therapeutic use in humans.
Summary Table
Disclaimer
For Research Use Only. Not intended for human or veterinary use. This compound is supplied solely for laboratory and R&D purposes.
Detailed Product Description
Epithalon is a stabilized synthetic tetrapeptide analogue of the endogenous pineal peptide epithalamin. It was developed to replicate and enhance the biological functions of pineal-derived factors that regulate aging and genome integrity. Preclinical studies have demonstrated that Epithalon activates telomerase in somatic cells through activation of telomerase reverse transcriptase, which promotes telomere elongation, and delays cellular senescence. These mechanisms are believed to underpin its geroprotective effects1. Epithalon has been extensively evaluated in aging-prone and cancer-prone rodent models, where it has been shown to reduce spontaneous tumor formation, suppress oncogene expression (notably HER-2/neu), and increase median and maximal lifespan1,2. The peptide also restores melatonin secretion rhythms in aged animals and stabilizes genomic integrity by reducing age-associated chromosomal aberrations. While not approved for human use, epithalon is actively used in laboratory research on aging, cancer biology, and radioprotection. It is intended solely for investigational applications involving cellular senescence, telomerase modulation, and epigenetic reprogramming in experimental models of aging and age-related disease3,4.
Research Highlights
Lifespan Extension:
Increased lifespan in CBA and SAMP-1 mice compared to controls1.
Antitumor Effects:
Reduced spontaneous and induced tumor growth in multiple murine models4.
HER-2/neu Suppression:
Decreased oncogene expression and tumor burden in transgenic mice4.
Radioprotection:
Promotes regeneration in radiosensitive organs post-irradiation (e.g., thymus, spleen).
Genomic Stability:
Lower incidence of chromosomal mutations in aging models3.
Circadian Regulation:
Restores melatonin rhythmicity in aged animals1.
Epithalon induces the expression and activity of telomerase reverse transcriptase in somatic cells, promoting elongation of telomeric DNA repeats at chromosomal termini. Telomere attrition is a hallmark of replicative senescence and genomic instability, particularly in highly mitotic tissues4. By sustaining telomere integrity, Epithalon enhances proliferative capacity, reduces the incidence of chromosomal aberrations, and preserves nuclear genomic architecture in aging cells. In senescence-accelerated murine models, TERT activation by Epithalon correlates with increased median and maximal lifespan, reduced incidence of cytogenetic anomalies in bone marrow metaphases, and improved resistance to oxidative and genotoxic stress2,4.
In transgenic FVB/N mice overexpressing the human HER-2/neu (erbB-2) oncogene, Epithalon administration results in a significant reduction in HER-2/neu mRNA levels, with a reported 3.7-fold decrease relative to saline controls. HER-2/neu encodes a receptor tyrosine kinase involved in mitogenic signaling via the MAPK and PI3K/AKT pathways and is implicated in the pathogenesis of multiple epithelial malignancies, including breast carcinoma. Epithalon’s suppression of HER-2/neu expression is associated with delayed tumor onset, reduced tumor multiplicity, and decreased tumor volume. These data suggest a transcriptional regulatory mechanism through which Epithalon modulates oncogenic signaling and suppresses neoplastic progression in HER-2-driven tumorigenesis4.
Pharmacokinetic Profile
Route of Administration
Subcutaneous
Dosing Frequency
Once daily
- Route of Administration: Subcutaneous injection
- Dosing Frequency: Once daily
- Half-Life: Not formally established in humans; estimated short plasma half-life typical of small peptides (minutes to low hours)2.
- Formulation: Lyophilized powder for reconstitution
Formulation & Handling
- Lyophilized peptide powder, reconstituted in sterile PBS or water.
- Store lyophilized peptide at –20?°C; upon reconstitution, aliquot and freeze at –80?°C to avoid degradation.
- Avoid repeated freeze–thaw cycles.
Selected Clinical Trial Activity
Epithalon is a research-grade compound that has been studied in laboratory settings but has not undergone full clinical development. It is not approved for therapeutic use in humans, and no large-scale clinical trials have been conducted to evaluate its safety or efficacy as a medication. Epithalon is supplied strictly for laboratory research and investigational purposes only.
References
Quality & Purity
This product is synthesized via solid-phase peptide synthesis (SPPS) and tested to ≥99% purity by HPLC with identity confirmed by mass spectrometry. A Certificate of Analysis (COA) is available for every batch. Learn about our full quality and testing process →
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