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Epithalon (CAS No. 307297-39-8), a synthetic tetrapeptide (Ala-Glu-Asp-Gly) with a molecular formula **C₁₄H₂₂N₄O₉** and molecular weight **390.34 g/mol**, is a key player in peptide-based gerontology. Developed by Russian scientist Vladimir Khavinson, it mimics the effects of epithalamin, a naturally occurring polypeptide in the pineal gland, and has gained prominence for its anti-aging and cellular rejuvenation properties .

Epithalon stimulates telomerase production, which maintains telomere length—the protective caps at chromosome ends that shorten with aging. By elongating telomeres, it delays cellular senescence, enhances DNA replication, and extends the lifespan of human somatic cells in vitro, overcoming the Hayflick limit . This mechanism underlies its geroprotective effects, including reducing age-related degenerative changes in the immune and neuroendocrine systems. Additionally, Epithalon regulates melatonin secretion, improving circadian rhythms and sleep quality while acting as an antioxidant to reduce oxidative stress and inflammation .

Preclinical studies highlight its potential in preventing age-related diseases such as cardiovascular disorders, dementia, and cancer, by inhibiting tumor growth and promoting apoptosis . In skin fibroblasts, it suppresses MMP-9 protein expression, associated with aging and pathological conditions. Commercially available as a **white, water-soluble powder** with ≥97% purity, Epithalon is produced via solid-phase synthesis and lyophilization, adhering to GMP and ISO standards . Major production hubs include Russia and China, where it is marketed for research purposes, particularly in anti-aging formulations, cosmetics, and nutraceuticals .

However, it remains unapproved by the FDA or EU for human therapeutic use, with current applications restricted to in vitro and animal studies . While generally well-tolerated, long-term safety requires further validation. Contraindications include pregnancy, active cancer, or hypersensitivity due to its potential impact on cellular proliferation . Ongoing research explores its epigenetic regulation of genes like **CCL11** and **HMGb1**, promising novel applications in neurodegeneration and age-related pathologies . As a frontier in peptide-based biotechnology, Epithalon exemplifies the intersection of synthetic chemistry and anti-aging research.

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