N-Acetyl Epithalon Amidate 20mg

N-Acetyl Epithalon Amidate

N-Acetyl Epithalon Amidate is a modified version of the synthetic peptide Epithalon (a.k.a. Epitalon). Epithalon itself is a component of naturally occurring cow pineal gland extract that is now produced synthetically. It is well known in research settings for its anti-aging properties and significant effects on cancer, infectious disease, DNA (primarily telomere) regulation, and skin health.

Even though Epithalon was discovered roughly forty years ago at the St. Petersburg Institute of Bioregulation and Gerontology, the peptide is still under active research and providing new insights. Most recently, scientists proposed potential epigenetic mechanisms to explain the influence that Epithalon has on neuronal differentiation of stem cells.

N-Acetyl Epithalon Amidate: Modifications

The modifications to Epithalon do not alter the peptide’s overall function, but they do alter the half-life, stability, and efficacy of Epithalon. Only two modifications are made to the native peptide: N-acetylation and amidation. Each has specific benefits that make Epithalon more potent and allow for lower dosing of the peptide.

Acetylation is a common, natural process that occurs to many proteins in the body. It is also a process used by the pharmaceutical industry to help a compound to reach the central nervous system. Acetylated molecules are much more capable of crossing the blood-brain barrier (BBB). Acetylation has been shown to increase the rate at which a compound crosses the BBB, thereby increasing the intensity of the compound’s effects and helping reduce the dosage of a compound required to achieve a specific outcome. Aspirin, for instance is the acetylated form of salicylic acid. Research shows that acetylation of salicylic acid increases the anti-inflammatory effects of the molecule.

Amidation is another natural protein modification that has been coopted by the pharmaceutical industry to improve the half-life of compounds. Amidated proteins are less sensitive to proteolytic degradation in the blood stream. They also tend to bind more strongly to their receptors, making amidation an excellent means of increasing potency and efficacy of a compound.

By altering Epithalon via acetylation and amidation, it is possible to increase the penetration of the peptide into the central nervous and protect it from degradation during the process. The result is increased potency of a given dose of Epithalon as well as increased efficacy of the compound due to improved receptor binding.

N-Acetyl Epithalon Amidate and the Brain

Research in cell culture shows that Epithalon influences gene expression in neurogenetic differentiation as well as protein synthesis. Molecular modeling suggests that occurs through epigenetic modulation of a handful of genes coding for the proteins Nestin, GAP43, β Tubulin III, and Doublecortin. Epithalon increases expression of these peptides by as much as 1.8 times via binding with specific histone proteins and allowing the genes to be accessed more easily[1]. The result of easier access to the DNA in those regions is increased expression of the genes and thus increased protein production.

The proteins being affected by Epithalon are important in the growth and development of neurons as follows.

• Nestin – This intermediate filament protein is expressed in nerve cells and plays an important role in the radial growth of axons. It also helps stem cells to differentiate into nerve cells, thus stimulating the growth of tissue in the central nervous system (CNS).
• GAP43 – GAP43 is often called the “plasticity” protein because plays important roles in neuronal growth cones during development and axonal regeneration. It plays critical roles in learning. Deletion of even one allele of the GAP43 gene leads to intellectual disability.
• β Tubulin III – This microtubule element is found in neurons and testis cells where it is involved in microtubule formation and oxidative stress responses. Research suggests that it is important in cellular adaptation to molecular stress and that deficiencies in this protein may play a key role in tumor aggressiveness.
• Doublecortin – Doublecortin is a microtubule-associated protein found in immature neurons. It is critical to the development of complex brain structures. Deficiencies in Doublecortin have been linked to double cortex syndrome in which a lack of migration of immature neurons leads to a smooth brain in males and misplaced neurons in females. The result of deficiency is profound intellectual disability.

By improving access to the DNA regions containing the genes that control the above proteins, Epithalon has been linked to improved learning, enhanced recovery from CNS injury, and potentially to reductions in the long-term effects of aging on the brain. This latter feature is just one of the many ways in which Epithalon has been found to positively affect the aging process. In particular, Epithalon has been shown to affect neuronal stem cell differentiation by promoting the growth and development of neurons from stem cell progenitors[2]. With a longer half-life and improved penetration in the CNS, the potency, and effects of N-Acetyl Epithalon Amidate will be enhanced compared to standard Epithalon.

N-Acetyl Epithalon Amidate and Skin Health

The ability of Epithalon to regulate gene expression patterns is hardly limited to the CNS. Research in skin stem cell cultures shows that Epithalon, even at very low concentrations increases proliferation of stems cells in rats regardless of age. In particular, fibroblast proliferation rates increase by as much as 45%[3].

It isn’t just the growth of fibroblasts that is affected, however. Research shows that Epithalon (and other short polyfunctional peptides) decrease rates of apoptosis and increase functional activity of fibroblasts[4]. This leads to “normalization” of the intracellular matrix. In other words, Epithalon restores homeostasis (biological balance) to the skin and helps to shift the balance in aging skin toward more youthful production of things like collage, elastin, and other proteins[4]. The net result is improved skin health. In fact, Epithalon has opened up a new field in research, referred to as gerontocosmetology, focused on skin health in age.

N-Acetyl Epithalon Amidate and Aging

Each of the above sections has dealt with a specific feature of Epithalon function, but each has also made note of the fact that Epithalon helps to restore DNA expression patterns in aging animals to those seen in younger animals. Indeed, restoration of youthful DNA expression patterns is the overarching theme associated with Epithalon. Production of this peptide by the pineal gland appears to decline with age, resulting in many of the age-related changes that impact health and longevity. Supplementation with Epithalon in insects and rodents has shown that Epithalon can decrease mortality by more than half and prolong life by as much as 27%[9].

The above changes in DNA expression patterns, possibly through epigenetic changes that result of histone protein binding, is at least part of the reason that Epithalon has such profound effects on aging. It is not the whole story though. Research shows that Epithalon also impacts antioxidant activity and telomere health.

In rat models. Injection of Epithalon has been shown to decrease LPO production and reduce oxidative modification of proteins[10]. LPO production (lipid peroxidation products) result from lipid peroxidation, which is a normal biological process known to production free radicals. LPO is necessary for several normal biological functions, such as the destruction of invading pathogens and the recycling of damaged proteins. The production of potentially dangerous free radicals is offset by the equal production of antioxidants. With aging, however, antioxidant production wanes thus cellular and protein damage from free radical production increases. Epithalon offsets the decline in antioxidant production and thus helps to maintain the homeostatic balance that prevents damage from free radicals.

Aging, in general, can be divided into several categories, but they are all interlinked. In general, DNA damage leads to protein malfunction. This, combined with direct protein damage, leads to cellular dysfunction. As cellular dysfunction accumulates, cells are either killed or become non-functional in a process known as senescence. Over time, both processes lead to tissue and organ dysfunction that eventually produces signs of aging like changes in sleep patterns, weight gain, wrinkling, greying of the hair, and increased incidence of chronic disease. The accumulation of this “macro-damage” is what eventually leads to death as the body becomes unable to sustain normal biological function. Epithalon helps to offset much of this dysfunction by regulating DNA and protein damage at a fundamental level.

N-Acetyl Epithalon Amidate: Summary

While Epithalon is not the single answer to halting the aging process, it does provide insight into how to counteract some of the foundational processes that lead to DNA and protein damage can help to thwart the overall aging process. According to Dr. Vladimir Khavison, the godfather of Epithalon development, as research into Epithalon continues, science gains a deeper, more nuanced understanding of what causes mammals, in general, and humans to age and eventually die. Epithalon is an important key to understanding how biochemical processes can be altered to slow or even halt some of the fundamental causes of aging. The development of N-Acetyl Epithalon Amidate is an important part of Epithalon research as its ability to penetrate the CNS will make it easier for researchers to explore the effects of Epithalon on aging in the brain. This will likely provide insight into how biochemical processes such as sleep and neuron growth affect learning, memory, cognitive resilience, and much more.

Storage Instructions:

All of our products are manufactured using the Lyophilization (Freeze Drying) process, which ensures that our products remain 100% stable for shipping 3-4 months reconstituted (mixed with bacteriostatic water) to maintain stability. After reconstitution, the peptides will remain stable for up to 30 days.

Lyophilization is a unique dehydration process, also known as cryodesiccation, where the peptides are frozen and then subjected to low pressure. This causes the water in the peptide vial to sublimate directly from solid to gas, leaving behind a stable, crystalline white structure known as lyophilized peptide. The puffy white powder can be stored at room temperature until you're ready to reconstitute it with bacteriostatic water.

Once peptides have been received, it is imperative that they are kept cold and away from light. If the peptides will be used immediately, or in the next several days, weeks or months, short-term refrigeration under 4C (39F) is generally acceptable. Lyophilized peptides are usually stable at room temperatures for several weeks or more, so if they will be utilized within weeks or months such storage is typically adequate.

However, for longer term storage (several months to years) it is more preferable to store peptides in a freezer at -80C (-112F). When storing peptides for months or even years, freezing is optimal in order to preserve the peptide’s stability.

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