Epithalon (also known as Epitalon) is a tetrapeptide isolated from bovine pineal gland extract in the 1980s by Professor Khavinson of the Institute of Bioregulation and Gerontology in St. Petersburg, Russia. Its amino acid sequence is Ala-Glu-Asp-Gly. It is the active core fragment of the natural pineal peptide Epithalamin and was later successfully synthesized.
In short, scientists discovered a substance in the pineal gland that can "rejuvenate cells," and Epithalon is the "smallest effective ingredient" of this substance. With a molecular weight of only 390.35 Da, it can bind to a specific DNA sequence (ATTTC) and regulate gene expression-a rare feat for small peptides.
Core Advantages and Functions
1. Telomerase Activation-"The Switch to Cell Lifespan"
Epithalon can upregulate hTERT mRNA expression, activate telomerase, and extend telomere length. First reported by Khavinson in 2003, and independently replicated and validated by Brunel University in 2025-it extends telomeres by an average of 33.3% in normal cells. This is the core basis for its designation as an "anti-aging peptide."
2. Restoring Circadian Rhythm-Without Exogenous Melatonin
It doesn't directly supplement melatonin, but rather repairs the pineal gland's ability to synthesize melatonin. Clinical studies show that urinary excretion of 6-sulfo-melatonin increased 1.6 times in elderly subjects, and the expression of circadian rhythm genes such as Clock and Cry2 was significantly improved.
3. Antioxidant and DNA Protection
It reduces the generation of free radicals in brain tissue, inhibits lipid peroxidation, and reduces the rate of chromosomal aberrations. In accelerated aging mice (SAMP-1), Epithalon's DNA-protective effect was even superior to melatonin.
4. Retinitis Pigmentosa-An Unexpected Clinical Highlight
A clinical trial involving 162 patients with retinitis pigmentosa showed an average improvement in visual acuity of 0.15–0.20, an expansion of visual field boundaries of 90–120 degrees, and a reduction or disappearance of absolute scotomas in 64.8% of patients. No adverse reactions were reported.
5. Animal Lifespan Extension Data – But Don't Get Too Excited
In CBA mice, the Epithalon group, which lived to 23 months, was four times longer than the control group; the longest-lived individual lived to 34 months (compared to 24 months in the control group). HER-2/neu transgenic mice also showed significantly extended lifespans. However, note that all animal experiments were conducted by Khavinson's team, and no independent laboratory has yet replicated these findings.
Storage (Lyophilized Powder Reagent Diameter)
Unreconstituted lyophilized powder: -20℃, sealed, protected from light + desiccant, stable for ≥24 months; for long-term archiving, store at -80℃, which can last for several years. It is hygroscopic; the N-terminal Glu will spontaneously cyclize into pyroglutamic acid, and heat and moisture accelerate this process.
Reconstituted: Dissolve in sterile water/BAC water/physiological saline, 2–8℃, protected from light, and use within 14–30 days (conservatively, 2 weeks is the most stable period); for longer storage, aliquot into single-use volumes at -80℃, but avoid repeated freeze-thaw cycles.
Before opening, allow the solution to equilibrate to room temperature for 15–20 minutes to prevent negative pressure from drawing moisture into the bottle and causing clumping.
Precautions
Pour water slowly along the side of the bottle, avoiding vortexing-although the tetrapeptide is short, its Glu-Asp is negatively charged, and shear force can promote cyclization/aggregation. The solution should be clear and colorless; if it becomes foggy or flocculent, discard it immediately.
Don't just look at "99% purity" for COA: AEDG is too low, and TFA/acetic acid counterion can falsely claim 10–15% apparent quality. Have the supplier confirm LC-MS (M+H)⁺ = 391.1, HPLC dual-wavelength (215/280 nm), and endotoxin data; otherwise, in cell experiments, if telomerase is not activated, you won't be able to distinguish whether the peptide is defective or the mechanism is malfunctioning.
It's just a RUO research compound, labeled "Research Use Only, not for human consumption"; the Russian clinic formulation is a different matter. The powder bought in the West isn't a legally injectable drug; it actually circulates in the body via IACUC.
When performing telomerase TRAP, a negative control of senescent cells without peptides and a known hTERT positive control are used. In Khavinson's raw data, cell passage number and serum batch number are hidden variables; without locking out the conditions, the intra-group CV would be terrifying.
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