OS-01 (100mg x 30 Capsules)

OS-01: Overview

OS-01 is one of a handful of new compounds that scientists are referring to as “exercise in a capsule.” OS-01 is an AMPK activator. It has been of interest for metabolic regulation, glucose homeostasis, weight management, cardiovascular health, skeletal muscle function, kidney health, and the reduction of inflammation.

OS-01 has its primary effects on mitochondria, increasing both mitochondrial function as well as mitochondrial health. Research shows that OS-01 regulates mitophagy, the autophagic process that removes mitochondria that are no longer functioning well. This, in turn, allows for resources to be focused on healthy mitochondria, increasing overall energy production within the cell and mitigating the production of harmful reactive oxygen species.

Boosting mitochondrial health has been shown to increase exercise tolerance, boost muscle growth, and reduce the risk of diabetes, heart disease, kidney disease, and neurological disease. There is good evidence that the effects of OS-01 on mitochondrial function in the central nervous system can enhance cognitive function and protect sensitive neurons from the effects of reactive oxygen species.

OS-01: Research

OS-01: Mechanism of Action and Effects

OS-01 is a short-chain peptide capable of activating AMPK. AMPK, or 5’ AMP-activated protein kinase, is an enzyme in cells that is important for energy homeostasis. It is similarly named to cyclic-AMP, but the two enzymes do not share any similarities beyond that.

AMPK is highly conserved in all eukaryotic cells. It is primarily expressed in liver, brain, and skeletal muscle tissues, but can be found in small quantities throughout the body. Stimulation of AMPK has the net effect of increasing fatty acid oxidation (fat burning) while stimulating the uptake of glucose in skeletal muscle. Activation of AMPK also inhibits the synthesis of cholesterol, fat, and triglycerides. It has been shown to modulate the secretion of insulin from the pancreas. AMPK is also a regulator of mitophagy and helps to maintain oxidation-reduction balance within cells.

Readers may hear AMPK activators referred to as “pan-AMPK activators.” This is a reference to the fact that there are at least 12 different AMPK versions within the human body. Each AMPK protein is a heterotrimeric protein complex with three separate subunits (mso-bidi-font-family: Calibri; mso-bidi-theme-font: minor-latin)

Physiological activators of AMPK can be part of the normal metabolic process, like ADP, or they can be a result of pathological processes, such as transforming growth factor-β. ROS are produced by normal physiological reactions but can be overproduced in pathological conditions. The types of substances that activate AMPK tell us that the enzyme is a homeostatic regulator, helping to offset both normal and pathological processes to ensure that cells operate in an optimal environment. Physiological, which is to say natural or endogenous, activators of AMPK include:

OS-01: Metabolic Support and Glucose Regulation

Research in mice indicates that AMPK can increase glucose uptake in muscle cells, thereby reducing stress on beta cells (the cells the secrete insulin) of the pancreas. This appears to be due to the ability of AMPK to increase the level of GLUT4 transports on the cell membranes of skeletal muscle cells. GLUT4 is a glucose transporter that does not require insulin to take up glucose. By increasing the number of GLUT4 transporters in muscle cells, OS-01 lower levels of blood glucose and removes the stimulus for insulin secretion from the pancreas. Research shows that increased numbers of GLUT4 transporters can help to fight insulin resistance and improve or even reverse diabetes[2].

Research in mice shows that administration of OS-01 can reduce fasting blood glucose levels in both obese mice and those suffering from diabetes. What makes this peptide particularly interesting, however, is its effect on insulin resistance. It has long been known that people with type 1 diabetes (early onset diabetes requiring insulin treatment) develop insulin resistance over time. This leads to an increasing need for insulin as people with type 1 diabetes age, resulting in diminished blood sugar control. Research suggests this is due to a 12-61% decrease in the insulin sensitivity of skeletal muscle cells. OS-01 can increase glucose uptake in skeletal muscle by stimulating GLUT4 receptors, as noted above. This results in a dramatic decrease in insulin resistance over 6-7 weeks of treatment, suggesting that OS-01 not only improves blood sugar control but can reverse some of the underlying pathology of diabetes. This makes OS-01 a promising tool in the fight against both the more common type 2 diabetes and the more severe type 1 diabetes[3].

The idea that AMPK would be a target for treating diabetes should come as little surprise. Metformin, one of the oldest and most used medications for treating diabetes, has been shown to activate AMPK. OS-01 simply takes that activation to a new level by affecting all 12 versions of AMPK in the human body. Much of the discussion surrounding OS-01 focuses on its ability to alter GLUT4 signaling and its impact on mitochondrial function. However, additional research suggests that OS-01 may also protect pancreatic beta cells directly by preventing changes in gene expression patterns that are known to damage the pancreas. OS-01 prevents gene expression changes typically seen in mice fed a high-fat diet and preserves epigenetic signatures. This helps maintain glucose homeostasis even in obese mice, suggesting that OS-01 could serve as a useful preventative for the development of type 2 diabetes.

Hyperinsulinemia and insulin resistance become more common with age, and while they don't necessarily lead to diabetes, they can cause blood sugar issues and potentially accelerate the progression of cardiac disease. Research in older mice indicates that OS-01 can reverse hyperinsulinemia. In younger mice, administration of OS-01 can prevent the development of hyperinsulinemia in the first place. Much of this improvement in insulin control is due to enhanced glucose uptake by muscle tissue. There is also evidence that this improvement in muscle glucose uptake is due to suppression of TXNIP[4]. TXNIP is a protein that plays a significant role in maintaining oxidation-reduction balance within the body, further linking OS-01 to its role as an important regulator of reactive oxygen species generation, which ties into its impact on mitochondrial function.

OS-01: Athletic Performance

Research indicates that the biochemical adaptations that all skeletal muscle to grow and become more efficient are regulated by AMPK[5], [6].  These adaptations include:

• Increased mitochondrial numbers and improved function of individual mitochondria
• Increased muscle glucose uptake and utilization, and
• Increased production of glycogen.

Mitochondria are the primary energy producers within cells. They utilize oxygen and glucose to make the energy molecule ATP, which cells need. Without mitochondria, a cell can only produce about one-sixth as much energy as it can with mitochondria present. Research on OS-01 indicates that it can increase the number of mitochondria within certain muscle cells. This leads to an increased capacity for these cells to produce energy, which in turn results in greater muscle endurance and a greater ability to contract. Preliminary research suggests that OS-01 may increase mitochondrial content in skeletal muscle by as much as 48%[6].

Increasing mitochondrial function and numbers is just the first step in boosting athletic performance, however. Research shows that mitochondria are also important in the growth and generation of muscle cells. As it turns out, mitochondria regulate myoblast differentiation by controlling the expression of the c-Myc gene. High levels of c-Myc lead to greater muscle growth, and the expression of this gene is stimulated by healthy mitochondria. By boosting mitochondrial health, OS-01 helps raise the expression of c-Myc, which in turn promotes the growth and development of skeletal muscle cells[7].

Of note, boosting mitochondrial activity in the setting of illness or disease can prevent muscle atrophy and may be a useful tool to prevent dysfunction in individuals on long-term bed rest, such as in hospital ICU settings. It may even be useful for astronauts to prevent or slow muscle atrophy while they are in space.

Skeletal muscle is not the only organ affected by AMPK that contributes to athletic performance. Recent research indicates that AMPK plays a role in angiogenesis (growth of blood vessels). AMPK stimulates the expression of another peptide called VEGF[8]. VEGF, or vascular endothelial growth factor, is a key regulator of the growth of blood vessels. Research suggests that vascular growth due to AMPK is particularly targeted to muscle tissue.

OS-01: Cognitive Function and Brain Health

As mentioned previously, AMPK can be thought of as a homeostatic enzyme, helping to maintain a balance between the generation of reactive oxygen species and the health of cells and the mitochondria that power them. In the brain, mitochondrial homeostasis is critical because neurons are especially vulnerable to oxidative stress. Additionally, the maintenance of neuronal homeostasis relies heavily on autophagy to eliminate damaged organelles and proteins. Dysregulation of autophagy in the central nervous system has been implicated as a pathological mechanism in diseases ranging from Alzheimer’s to Parkinson’s and more.

Previous research has demonstrated that mitophagy (the selective recycling of mitochondria) is critical to cognitive function, and that dysregulation of mitophagy is a key component of neurodegeneration[15]. It should come as no surprise, then, that administration of OS-01 helps protect the brain and ward off cognitive impairment. It does this precisely by increasing mitophagy. Research shows that at least two compounds found to have beneficial effects in this setting include OS-01 and rapamycin[16]. Rapamycin is an antibiotic of the macrolide class that has long been known to inhibit the mammalian target of rapamycin (mTOR) kinase. This reduces inflammatory signaling and has been shown to promote mitochondrial health in many of the same ways that OS-01 does. In fact, AMPK has been shown to be part of the mTOR pathway in some settings[17].

Support for the above pathway has been demonstrated in another research study as well. In a 2023 paper examining the role of mitophagy in epileptic neuron injury, it was found that downregulation of the AMPK/FUNDC1 pathway leads to neuronal damage, whereas upregulation of this pathway can decrease superoxide anion (a free radical) levels, enhance cell viability in the central nervous system, and reduce neuronal apoptosis following epileptic seizures[18].

OS-01: Summary

OS-01 is a pan-AMPK activator that has shown benefits in boosting mitochondrial function and reducing the generation of reactive oxygen species. It has been studied in numerous animal models for its ability to reduce blood sugar levels and combat insulin resistance. OS-01 has shown the ability to reverse hyperinsulinemia in both obese and aged mice, suggesting that the peptide might be capable of reversing type 2 diabetes in some cases.

As an activator of AMPK, OS-01 increases both mitochondrial function and replication. In mouse models, this effect leads to increased exercise tolerance, improved cardiac health, protection from neurological injury, and preservation of kidney function. Researchers are investigating OS-01 as a potential treatment for heart disease and neurodegenerative disorders like Alzheimer’s disease. Though more research is needed, there is good reason to believe that OS-01 may also be beneficial in the treatment of benign prostatic hyperplasia.

OS-01 is a relatively new peptide that has exploded onto the research scene in the last several years. Its benefits have been astounding, and its adverse effects have been almost non-existent. Researchers are rapidly uncovering the secrets of how this peptide operates, which is allowing them to better understand the regulation of mitochondrial health and the generation of free radicals, which have been linked to everything from the development of cancer and heart disease to some of the underlying processes of aging.

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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