N-Acetyl Epitalon Amidate

Technical data

INN name

N-Acetyl Epitalon Amidate

Molecular formula

C16H25N5O9

Molecular weight

431.40 g/mol

Identity and composition

El N-Acetyl Epitalon Amidate is a postulated synthetic derivative of Epitalon (AEDG), a tetrapeptide of the family of short peptide bioregulators that is investigated in preclinical models for its proposed geroprotective, neuroprotective and neuroendocrine effects. It is offered exclusively as laboratory material.

Product for research use.

As for its chemical identity, the consulted literature has no confirmed values in reference databases (PubChem/DrugBank): there is no reported CAS, molecular weight ni molecular formula verified for the derivative (the values that circulate in catalogs actually correspond to the base Epitalon and are incompatible with acetylation and amidation, so they are omitted here).

La sequence is described as Ac-Ala-Glu-Asp-Gly-NH2, a derivative postulated from the name; the N-terminal acetyl (Ac-) and C-terminal amide (-NH2) ends are inferred from the nomenclature, not from a structural source. The parent peptide, Epitalon, corresponds to the sequence Ala-Glu-Asp-Gly (AEDG), confirmed in peer-reviewed literature (PMID 32019204).

Synonyms: N-Acetyl Epithalon Amidate, N-Acetyl-Epitalon-Amidate, acetylated/amidated Epitalon (derivative).

Mechanism of action

It is important to note that there is no specific primary literature on the N-acetylated/C-amidated derivative; the available mechanistic data correspond to the Epitalon base (AEDG) and are presented here for educational purposes only.

For Epitalon, several mechanisms have been proposed, investigated mainly in vitro:

• Telomerase and telomeres: telomerase activation and telomere elongation observed in vitro in human fibroblasts (PMID 40141333).

• Epigenetic mechanism: preferential binding to histones H1/6 and H1/3 and to specific DNA sequences, associated with an increase in the transcription of neurogenic genes such as Nestin, GAP43, beta-tubulin III and Doublecortin, with increases on the order of 1.6 to 1.8 fold in mesenchymal stem cells (PMID 32019204).

• Pineal neuroendocrine regulation: proposed modulation of melatonin synthesis through AANAT and pCREB (PMID 40141333).

It is theorized that N-terminal acetylation and C-terminal amidation would increase stability against exopeptidases, but this is not documented in primary sources for this compound. A 2025 review emphasizes that the precise mechanism of action of this tetrapeptide remains unverified (PMID 40141333).

Pharmacokinetics

Not available. No peer-reviewed source reports a half-life or pharmacokinetic parameters, neither for the base Epitalon nor for the N-acetyl amidated derivative. It is not possible to offer numerical values of absorption, distribution, metabolism, or elimination without falling into speculation. Any pharmacokinetic characterization would have to be generated experimentally within the research protocol itself.

Scientific evidence

The available evidence is preliminary and limited to base Epitalon, not the N-acetyl amidate derivative, which appears only in the catalogs of 'research chemicals' suppliers without studies of its own.

For Epithalon there are relatively extensive in vitro and in vivo studies in animal models (mice, rats, flies and monkeys). In humans the evidence is scarce and limited: the consulted literature mentions a trial in patients with retinitis pigmentosa (n=162) and a study on effects on circadian rhythm in women (n=75) (PMID 40141333).

No trials registered in modern regulatory phases (FDA/EMA) were identified, nor approval as an API, nor records on ClinicalTrials.gov for the derivative. The indications explored —geroprotection/longevity, neuroprotective, antioxidant and neuroendocrine effects— are all at the preliminary and a 2025 review highlights important information gaps (PMID 40141333). The overall confidence level of these data is low.

Research applications

Product for research use.

It may be of interest for research in:

• In vitro studies on telomerase activity and telomere dynamics (cell lines).
• Preclinical models that explore epigenetic mechanisms and markers of neurogenesis.
• Comparative work on enzymatic stability against native Epitalon, given that the argument of greater resistance to exopeptidases is unverified experimentally.
• Exploratory neuroendocrine research (e.g., melatonin-linked pathways) in appropriate models.

Not applicable for:

• clinical use, clinical use, diagnostic or therapeutic.
• Any application that depends on efficacy or safety data in humans for this derivative, since none exist.
• Formulation of supplements or products for public sale.

Research protocols

The literature reviewed does not contain specific study doses for N-Acetyl Epitalon Amidate, so it is not possible to indicate dosing ranges supported by the available evidence. The derivative has no trials of its own and the cited sources describe mechanisms of the base Epitalon without dosing protocols transferable to this material.

In view of the above, any dose-response design must be defined by the investigator within their own validated protocol, starting from appropriate methodological references and not from unverified commercial values. The presentations offered are of 5 mg y 10 mg of lyophilized peptide.

Reconstitution

As a general standard laboratory guide, lyophilized peptides of this type are usually reconstituted with bacteriostatic water (sterile water with approximately 0.9% benzyl alcohol as preservative), which allows the solution to be kept for several days under refrigeration.

General steps:

• Let the vial and the diluent reach room temperature before opening.
• Add the bacteriostatic water slowly, letting it run down the inner wall of the vial, without injecting directly onto the powder.
• Do not shake: gently swirl the vial until fully dissolved.
• Adjust the diluent volume according to the working concentration desired for your protocol (the larger the volume, the lower the concentration per unit volume).

For single-use or very short-duration studies, sterile water for injection can also be used; bacteriostatic water is preferable when repeated withdrawals from the same vial will be made.

Stability and storage

As standard laboratory handling practice:

• Lyophilized (powder): is the most stable form. It is best preserved protected from light, moisture and heat. Storage under refrigeration or, for prolonged periods, freezing, helps maintain the integrity of the peptide.

• Reconstituted (in solution): must be kept under refrigeration and used within a short window of time. For more prolonged preservation, freezing is usually preferred, avoiding as much as possible the repeated freeze-thaw cycles, which can degrade the peptide.

Always handle with aseptic technique and label the vials with the reconstitution date. These are general handling recommendations; no specific stability studies are available for this derivative.

Safety profile

There are no specific safety data for the N-acetyl amidate derivative in the consulted literature. The 2025 review explicitly identifies a critical safety-information gap for this class of peptide and notes that, before eventual approval as an API, additional studies on short- and long-term toxicity are essential (PMID 40141333).

In the absence of a documented toxicological profile, no contraindications, interactions, or tolerance margins can be established for this material. It must be handled with the general precautions applicable to any uncharacterized research reagent: use of personal protective equipment, avoiding exposure, and restricting its use to personnel trained in a controlled laboratory environment. It is not intended for clinical use.

Comparative context

N-Acetyl Epitalon Amidate belongs to the class of the short peptide bioregulators by Khavinson, developed at the Institute of Bioregulation and Gerontology in St. Petersburg.

Compared to the Native Epitalon (AEDG), the N-acetyl amidate variant is marketed on the premise of greater enzymatic stability, attributed to the blocking of the N-terminal and C-terminal ends. This is a pharmacologically plausible argument, but not experimentally verified in the literature.

It shares the postulated target —telomerase and epigenetic mechanisms— with the Epithalamin, the bovine pineal extract from which Epitalon was originally derived. In summary: the same conceptual lineage and the same mechanistic hypothesis as the parent peptide, with the declared (but not demonstrated) difference of greater resistance to exopeptidases.

History and development

The compound falls within the line of Russian research on short pineal peptides initiated with the Epithalamin, an extract of the bovine pineal gland. From that extract the Epitalon (AEDG, Ala-Glu-Asp-Gly), a synthetic tetrapeptide studied as a bioregulator within the Khavinson school, at the Institute of Bioregulation and Gerontology in Saint Petersburg.

El N-Acetyl Epitalon Amidate represents a proposed subsequent modification to that structure, with N-terminal acetylation and C-terminal amidation theoretically oriented toward improving stability. Unlike the base Epitalon—which has preclinical studies and some limited human reports (PMID 40141333)—this derivative appears only in catalogs of research reagent suppliers, without its own studies or associated regulatory records.

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Certificate of analysis per batch

Batches of N-Acetyl Epitalon Amidate with a certificate of analysis published in the COA catalog:

• Lot EXO010626129A — 10 mg, issued 2026-05-28
• Lot EXO010626129B — 5 mg, issued 2026-05-30

Scientific references (3)

Peer-reviewed literature on N-Acetyl Epitalon Amidate, with its PubMed identifier when available:

• Peptide bioregulators inhibit apoptosis (Khavinson VKh, et al. · Bulletin of Experimental Biology and Medicine · 2000) — Study on the anti-apoptotic effects of Epithalon and its role in telomeres. PMID 11276315.
• Epithalon peptide induces telomerase activity and telomere elongation in human somatic cells (Khavinson, et al. · Bulletin of Experimental Biology and Medicine · 2003) PMID 12937682.
• Overview of Epitalon-Highly Bioactive Pineal Tetrapeptide with Promising Properties (Araj, et al. · International Journal of Molecular Sciences · 2025) PMID 40141333.

Otras presentaciones de Amidato de N-Acetil Epitalon

• Epitalon

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