CJC-1295 vs Sermorelin: What to Know in 2021

CJC-1295 vs Sermorelin: What to Know in 2021

CJC-1295 vs Sermorelin: both Sermorelin and peptide CJC-1295 are the derivatives of growth hormone-releasing hormone (GHRH) and are often compared to one another in terms of their properties and functions. In addition to the number of similar actions that they share, both CJC-1295 and sermorelin also have differences. For the desired application, the choice of the best peptide depends more on the differences between them rather than the similarities that they share.

The Structure of CJC-1295 vs Sermorelin

Sermorelin is also known by the name GHRH 1-29, which means that the first 29 amino acids from a large growth hormone-releasing hormone, is sermorelin. The structure of CJC-1295 also consists of the first 29 amino acids of GHRH, but the difference is that there is a modification in some of the amino acids.

The Structure of CJC-1295

Sequence: Tyr-D-Ala-Asp-Ala-Ile-Phe-Thr-Gln-Ser-Tyr-Arg-Lys-Val-Leu-Ala-Gln-Leu-Ser-Ala-Arg-Lys-Leu-Leu-Gln-Asp-Ile-Leu-Ser-Arg

Molecular Formula: C152H252N44O42

Molecular Weight: 3367.954 g/mol

The Structure of Sermorelin

Sequence: Tyr-Ala-Asp-Ala-Phe-Thr-Asn-Ser-Tyr-Arg-Lys-Val-Leu-Gly-Gln-Leu-Ser-Ala-Arg-Lys-Leu-Leu-Gln-Asp-Met-Ser-Arg

Molecular Formula: C149H246N44O42S

Molecular Weight: 3357.933 g/mol

GRF (1-29) which means the growth hormone-releasing factor (1-29) is another name for Sermorelin. The modified form of GRF (1-29), which is sometimes known as Mod GRF (1-29) or tetrasubstituted GRF (1-29) is another name for CJC-1295. The potency of the first 29 amino acids of GHRH is the same as the potency of the full 44 amino acids of GHRH, but the natural metabolic clearance processes of the body clear it very rapidly. To decrease the rate of clearance and thereby boost the half-life, sermorelin was modified so that CJC-1295 can be made more resistant to enzymatic cleavage. Research studies indicate that sermorelin’s half-life is somewhere around five minutes while the half-life of CJC-1295 is 30 minutes.

The Argument for CJC-1295 DAC

The modification in CJC-1295 is often done by adding a lysine residue and DAC, i.e., a chemical structure, to the carboxy-terminal end. DAC means drug affinity complex. The role of DAC is mainly to help bind the molecules that it is attached to, with the blood protein albumin. This action helps them in extending the half-life of these compounds and also in extending their duration of action. With DAC, the time of total clearance of CJC-1295 can roughly increase from 1 hour to more than 96 hours.

Although different scientists of this field are giving different opinions on whether the name CJC-1295 is used only for mod GRF (1-29) with DAC added or whether the “DAC” component must be specified since mod GRF(1-29) and CJC-1295 can be used interchangeably. The CJC-1295 is considered to be inclusive of DAC by the original developer. In other words, it can be said that when someone says “CJC-2195” they simply mean mod GRF (1-29) with DAC added to it. Many people specify CJC-1295 with DAC simply to make it clear. In this article, the CJC-1295 mentioned refers to the modified version of mod GRF in which DAC is added.

Plasma Growth Hormone: CJC-1295 vs Sermorelin

The levels of Growth Hormone in the blood are raised by using both the sermorelin and CJC-1295, by the stimulation of the growth hormone-releasing hormone receptor in the anterior pituitary gland. Since both Sermorelin and CJC-1295 operate at the level of the receptor of GHRH, they preserve the normal pulsatile function of Growth Hormone secretion. However, if we talk about one amongst the two, then it is sermorelin that provides the more natural ebb and flow of Growth Hormone because it gets cleared from the body much faster as compared to CJC-1295. The best way to explain the two peptides and their effects on the Growth Hormone curve is that the Growth Hormone levels are raised by both and also both raise the relative preserving peaks and troughs, while the overall amount of time spent at the higher Growth Hormone levels is extended by CJC-1295. In other words, we can say that the sharp peaks are turned into plateaus to some extent by the CJC-1295. With this, the effects of Growth Hormone are boosted substantially and the physiology is also altered to some degree. Still, one of the main reasons to prefer Sermorelin over the peptide CJC-1295 is that the most natural ebb and flow pattern is provided by Sermorelin.

Disclaimer: The products mentioned are not for human or animal consumption. All the information shared in this article is for educational purposes only.

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Oral Peptides – Fact or Fiction?

Oral Peptides – Fact or Fiction?

Over the past decade, due to their various applications, peptides have enjoyed a great upturn in the production pipeline in biotechnology and pharmaceutical companies. The advantage of being more selective over the small molecule drugs have been shown by the peptides due to their highly specific functions in the body that cannot be mimicked by simple chemical compounds and as a consequence of the greater number of its interaction with the target, the peptides have shown very less off-target effects and increased potency. In addition to this, the peptides usually have low immunogenicity, lower overall systemic toxicity, and are usually well-tolerated since the body naturally produces peptides.

The administration of peptides via the oral route has become considerably more attractive with its significant improvements in the delivery methods. Better patient compliance is observed via oral administration. In addition to the medicines, Linzess (linaclotide) and Trulance (plecanatide), that have led the oral peptide delivery wave, many other peptides with the same administration route are also being developed. Molecules like Ozempic (semaglutide) which have been previously approved as an injection for the treatment of metabolic disease (Type II Diabetes), are now in the last phase of Clinical Testing using an Oral Route of administration. The working mechanism of these drugs is based on the interaction with the receptors present on the surface of the pancreatic beta cells to stimulate the release of insulin for diabetes. In addition to this, the pharmaceutical industry has also moved towards rare diseases and the orphan drugs have also been extended to peptides which are further targeting inflammation and infectious diseases.

A large capacity manufacturing will be required as metabolic diseases are at record levels around the world. Since the absorption rate of these molecules is very low in the small intestine, the challenge associated with the oral delivery will be the requirement of the material in large quantities as the growth of such drugs is really strong.

Peptides and proteins are high molecular weight biopolymers and consist of both hydrophobic and hydrophilic appendages in their structure. Because of these properties, the peptides are not easily absorbed by the intestine. In addition to this, due to the digestive roles of the duodenum and stomach, they are degraded due to which they might not even be available for absorption by the intestine. In simple words, when ingested, peptides are recognized as food by our bodies.

Due to these barriers, the parenteral route is the most common route of administration used for the peptide drugs, of which approximately 75% is given via intramuscular, intravenous, and subcutaneous injections. Although this route is appreciable, the inconsistent blood drug concentrations, frequent injections, and low acceptability by the patients make the parenteral administration a less desirable approach. To overcome this, the drug developers are trying to approach the oral route of administration for the peptides. Most of the drugs available in the market are either given as capsules or pills, thus representing the forms that most of the patients prefer.

Challenges and Opportunities for Oral Peptides

Numerous obstacles need to be overcome for successful delivery via the oral route. The first target that the developers should take into consideration is the selection of the peptides that are appropriate for the oral route of administration. After this, the first obstacle that needs to be taken care of is the sustainability of the oral formulation in a highly acidic stomach environment. The next is that the design of the formulation must promote dissolution in the small intestine’s high pH environment and also protect the peptide from the protease enzyme’s degradation. After all this, the peptide must be absorbed into the comparatively impermeable epithelium of the intestine.

Even if these obstacles are removed, it will not be possible to administer the peptides via the oral route until therapeutically relevant bioavailability is achieved.

Despite the challenges, the orally administered peptide therapeutics have high potentials. The biggest example is the ongoing production of the oral leuprolide tablet that is used in treating endometriosis. It is one of the most common gynecological disorders and in the US, approximately 6 million women are affected by it. Currently, leuprolide, effective treatment for endometriosis, is administered via the parenteral route which limits its use because of the irreversibility of the depot injection, which sustains in the body for around 30 to 90 days and the injection also causes inconvenience and pain.

For the patients, a daily oral leuprolide tablet has proven to be an effective and friendly alternative to the monthly depot injections. The oral route has also motivated the patients to use more frequent and earlier medication.

Disclaimer: The products mentioned are not for human or animal consumption. All the information shared in this article is for educational purposes only.

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Oxytocin – The Love Hormone

Oxytocin, which is also known as the Love Hormone, is a constitutionally developing peptide hormone and neuropeptide made in the hypothalamus and liberated by the posterior pituitary gland. Biologically, it is liberated during the birth of a child and helps in stimulating the uterine contractions during labor assisting in delivering a baby. After the baby is born, this hormone plays a significant role in social bonding between the mother and the child and also stimulates lactation in the mother. This “bonding activity” is the one due to which the “Love Hormone Connotation” has risen.

Oxytocin is comparatively a small 9 residue peptide that consists of a single disulphide bond and it is the 1st synthetic peptide to be developed for human utilisation. In 1906, Dale was the one to originally isolate this peptide. In the early 1950s, Victor du Vigneaud did the successful sequencing and then afterwards synthesized it. In 1955, for the work conducted on Oxytocin, Victor du Vigneaud was also awarded the Nobel Prize. Oxytocin is a peptide that is sustained and is found overall in the vertebrate species.

During Childbirth, Syntocinon or Pitocon, the Synthetic Oxytocin, is prescribed regularly to induce and augment labour. Rapid heartbeat and unusual bleeding are sometimes observed as the side effects. In 1998 it was evaluated by the Journal of the American Medical Association that in the US, 16% of the labors are induced and an additional 16% of labors that initiate instinctively are supplemented with the inducing drugs. Just post-birth, Oxytocin is also applied to avert postpartum hemorrhage if the contraction of the uterus is not continued and the bleeding is not stopped. Oxytocin can rupture the uterus if it is delivered in too much quantity and top rapidly.

The Nasal Spray formulation of Oxytocin is sometimes, although rarely, provided to the mothers having difficulty with milk let-down in the initial few days of nursing.

Because of the impersonating roles of Oxytocin in childbirth and nursing, researchers have observed Oxytocin for many years, primarily as a pregnancy hormone. In addition to this, it can also be used to induce termination or complete a miscarriage.

In many recent studies, scientists have revealed numerous effects of Oxytocin in both men and women. Oxytocin has shown much more pleiotropic effects than the realisation of the scientists. A wider role of Oxytocin was suspected by the scientists when they observed that the receptor reaching high concentrations in the laboring uterus is also found in other tissues like the reproductive tract, heart, and brain, in both women and men. In addition to this, many researchers also suspect that there are one or more than one Oxytocin receptors that are still unidentified. In the brain, Oxytocin is shown to play a large and unexplored role. In addition to being a hormone that is circulated in the bloodstream, it is also a neurotransmitter that travels in the brain’s nerve cells and at another place also. Cells of the hypothalamus make oxytocin and transfer it to the pituitary gland and also to the different regions of the brain. Moreover, oxytocin is not only produced by the cells of the hypothalamus but the heart, testicles, ovaries, and blood vessel walls have also shown to make their own oxytocin. Some research studies have also shown that oxytocin might help benefit people with Anxiety, Autistic Spectrum Disorder (ASD), and Irritable Bowel Syndrome (IBS).

Oxytocin is The Love Hormone?

Oxytocin is not only associated with childbirth and lactating mothers but the researchers in 2012 have also shown that people who are in the initial stages of romantic attachment have higher levels of oxytocin than those who are non attached and single and the levels have been shown to persist for at least 6 months. The release of oxytocin is stimulated during sexual activities. Some studies have shown that in women the reason behind this might be the increased uterine motility to help sperm reach their destination.

In addition to the effects of oxytocin in the uterus and lactation, it has also been shown to impact social, cognitive, and emotional behaviours when released in certain parts of the brain. Some research studies have shown the impacts of oxytocin on pro-social behaviours and emotional responses that contribute to trust, relaxation, and psychological stability. In the research studies in several species, it has been observed that brain oxytocin reduces stress responses, including anxiety.

Disclaimer: The products mentioned are not for human or animal consumption. All the information shared in this article is for educational purposes only.

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Selank for Brain Health and Memory

Selank for Brain Health and Memory

With our evolution and changes, the brain also undergoes the same on the basis of different factors like our experiences, the amount of sleep that we get, and the food that we eat. We usually worry about our physical health but not much about mental health, which forces us to understand the importance of nootropics and selank.

What are Nootropics?

The word is derived from Ancient Greece and means ‘turning of the mind’. These are a type of supplement which assist in the enhancement of the cognitive function in a person. Basically, nootropics benefit the people facing learning and memory issues as these substances enhance motivation, creative ideas, and memory.

What is Selank?

It is a type of nootropic, anxiolytic peptide, i.e., it belongs to both the nootropic and the peptide category. Most the people use this compound to inhibit anxiety.

The Institute of Genetics of the Russian Academy of Science developed this compound, which was earlier known by the name TP-7. A combination of a sequence of tuftsin and a stabilizing compound makes Selank.

The tetrapeptide tuftsin is known for its immunostimulatory effects, i.e., it stimulates the immune system by activating several components.

Selank is also known for its antidepressant and antiasthenic properties. Asthenia is a kind of disorder in which the person experiences an overall lack of energy or physical weakness.

Selank vs Semax

There is another compound known as Semax which is similar to Selank and comes from a different hormone in the brain. It has a different working mechanism, i.e., it enhances circulation and helps in preventing liver damage.

How Selank affect your brain?

One of the greatest muscles in our body is our mind. The brain is active even when we sleep. It does not get any holiday or breaks, so taking care of our brain is very essential.

The effectiveness of Selank on regulating the brain-derived neurotrophic factor was tested in rats, where for the duration of 30 weeks, each rat was given 10% ethanol as their only source of fluid. The results of the study demonstrated the effect of Selank on the age-related disturbances formed as a consequence of chronic alcohol intoxication.

Benefits

One of the most beneficial effects of Selank is against Anxiety, as it can limit the amount of anxiety faced by an individual. In addition to this, since it is also a nootropic, it helps in the enhancement of memory and learning.

Studies are also underway to analyse the effect of Selank in treating brain damage recovery. For now, no side effects are found to be associated with this compound, which makes it a safer option for use over the other alternative substances.

Selank – Bodybuilding Dosage

Selank is usually taken via 2 methods – one is in liquid form through injection into the skin subcutaneously. For this, it is usually available in the form of lyophilized powder to which sterile water or bacteriostatic water needs to be added. The other less common variation is in the form of a nasal spray.

Lyophilized Powder

The compound in this form needs to be reconstituted using sterile or bacteriostatic water. The important point that needs to be kept in mind for this is that the water needs to be added via the side of the vial and not simply sprayed onto the powder. The dosage needs to be kept at 0.1ml per day.

Another important point that needs to be kept in mind is that it has more neurorestorative properties which means that it has the potential to reverse brain degeneration so as to protect the newly regenerated cells.

Nasal Spray

The dosage in the case of nasal spray is simple and straightforward, i.e., one spray per nostril in a day. This dosage is expected to show the best results. So in a month, only about 3 ml of spray would be needed.

Although nasal sprays are not considered to be the most effective ones, still these can be preferred in cases where a person is afraid of needles. However, the lyophilized version shows a better and direct effect.

So to conclude, it is as important to take care of mental health as it is of physical health. So take care of the brain in a better way by using these supplements and thereby enhance the memory.

Disclaimer: The products mentioned are not for human or animal consumption. All the information shared in this article is for educational purposes only.

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Peptides Reconstitution

Peptides Reconstitution

In this article, you’ll find out how peptides reconstitution works. Peptides are short stretches of amino acids which are better known as the building blocks of proteins. Peptides often mimic the function of important proteins or hormones and help to establish the positive effects of the same without any adverse effects. Among the various significant functions of peptides include boosting physiological metabolism, weight loss, enhancing cognitive function, improving sleeping patterns and sexual health. Of late, many peptides have been approved for human consumption especially those regulating metabolism of body fat.

Lyophilized Peptides

The manufacturers sell peptides in freeze-dried powder or lyophilized form. Lyophilization is the technique whereby water gets removed from a solution upon freezing. The use of vacuum allows ice to be directly converted into vapor from solid without passing through the intermediate liquid phase. The powder either has a granular appearance or looks fluffy depending on the technique used for lyophilization.

Peptides Reconstitution

The lyophilized peptides need to be dissolved in the solvent before use. There is no universal solvent that can be used for all the peptides. The choice of solvent is guided by peptide stability and compatibility of the specific solvent with bioassays. In this respect, sterile water or bacteriostatic water often is the first choice of solvent. In spite of being the first choice, sterile or bacteriostatic water cannot dissolve every peptide. Hence experimentation with different solvents is often required for optimizing the solvent of choice. Sodium chloride solution in water is not advised to be used for dissolving peptides so as to avoid precipitation with acetate salts.
The polarity or native charge of a peptide is the key determinant for the solvent of choice. Basic peptides require acidic solvents whereas acidic molecules require basic solvents for optimal dissolution. The hydrophobic and neutral molecules dissolve best in organic solvents like DMSO, propanol and acetic acid. The powder should be dissolved in a small volume of the organic solvent and further diluted in sterile water. Important to note is that peptides with methionine or free cysteine should not be d in DMSO to avoid side-chain oxidation else they are rendered inactive.

Peptides Reconstitution Guidelines

Selection of appropriate solvent demands use of sterile water, 0.1% acetic acid, or any solvent which can be easily removed by lyophilization. It is recommended to dissolve a small amount of the peptide in the chosen solvent before dissolving the complete vial. The molecule should always be dissolved to form a higher stock concentration than that required for the actual assays. It can be diluted further in the appropriate assay buffer to derive at the appropriate concentration for use in the bioassays.

Sonication

Upon resuspension, sometimes visible particles persist in the peptide solution. The vial can then be sonicated to enhance the dissolution of the particles to yield a clear solution. Sonication does not modify the solubility of the peptide but expedites the breaking up of the particles to enhance solubility. Post sonication, the researcher has to inspect for the presence of any surface layer, cloudy appearance, or gel-like consistency. If so, then the peptide has merely got suspended but not dissolved. Hence, it would demand use of a stronger solvent.

Practical Implementation in the Laboratory

In this segment, we have outlined simple guidelines for the effective dissolution of peptides in the laboratory. Most peptides have recommended storage temperatures as lyophilized powder and solution and should be adhered to. If the powder form of the drug is stored in refrigerated condition, it should be equilibrated to room temperature initially before resuspension. The peptide solution can be filtered through a 0.2 µm filter to avoid any possible bacterial contamination since it is a rich source of amino acids.

Peptides Reconstitution – Example using sterile water as the diluent:

Step 1 – The plastic cap from the peptide vial should be removed so that the rubber stopper can be accessed.

Step 2 – The rubber stopper of the sterile water vial gets exposed upon removal of the plastic cover of the vial.

Step 3 – The rubber stoppers should be swabbed with alcohol to sterilize them from any possible bacterial contamination.

Step 4 – 2mL (milliliters) of water needs to aspirated from the sterile water vial.

Step 5 – 2mL (milliliters) of sterile water needs to be injected into the peptide vial, allowing the water to enter the vial gradually.

Step 6 – The vial should be gently swirled to allow the peptide to dissolve into the solvent. Shaking of the vial should be avoided.

Disclaimer: The products mentioned are not for human or animal consumption. All the information shared in this article is for educational purposes only.

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Tesamorelin: The Game Changer

Tesamorelin: The Game Changer

Fitness-conscious people often face the challenge of losing fat from the abdomen. Even strict food regimes and exercise do not help to lose truncal obesity. With the advancement of medical knowledge, a new peptide called Tesamorelin is now available to help overcome stubborn fat with minimal adverse effects on the body.

What is Tesamorelin?

Tesamorelin is a synthetic analog of growth hormone-releasing hormone (GHRH) and comprises 44 amino acids and a trans-3-hexenoic acid group. The peptide promotes weight loss and can be used with medical recommendations only. Theratechnologies was the first organization who manufactured the peptide with the brand name of EGRIFTA.

The importance of growth-hormone-releasing-hormone

The hypothalamus in the brain secretes GHRH. Hypothalamus is a significant gland that regulates diverse physiological functions including hormonal release and regulation of body temperature. The secreted GHRH in turn stimulates the release of growth hormone (GH) from the pituitary gland of our body.

The efficiency of the peptide depends on the amino acid composition of GHRH combined with 3-hexanoic acid moiety. The moiety works like a plant metabolite and hence is safe for ingestion. Tesamorelin was approved for use in November 2010. The peptide helps to lose fat in HIV patients as the antiretroviral drugs often induce lipodystrophy. Bodybuilders and fitness enthusiasts also use it to lose abdominal fat upon regular use.

How does Tesamorelin work?

The peptide just like its natural counterpart promotes the release of GH from the pituitary gland. GH in turn promotes lipolysis or metabolism of stored lipids and triglycerides in the body. Lipids and triglycerides are versions of fat that are stored in our body for a future source of energy. Hence high levels of the same increase risk of cardiac disease. Tesamorelin reduces visceral fat around the abdomen. Studies on HIV patients with lipodystrophy show that the molecule can reduce abdominal fat by about seventeen percent within twenty-six weeks. It also decreases liver fat by up to eighteen percent.

The recommended dose of Tesamorelin in average adults is 2 mg each day. It can be injected beneath the naval region while avoiding any region of scarring or bruising. The drug should be used immediately upon reconstitution. The lyophilized drug can be stored between 36 and 46 degrees Fahrenheit. The peptide solution should be used only if it is clear and free of particles upon reconstitution.

Other Lesser Known Benefits of Tesamorelin

The peptide not only improves the body’s natural ability to secrete GH but also has far less side effects compared to other GHRH secretagogues. The peptide reduces belly fat as well as confers additional benefits. It has been found to improve cognitive function on individuals aged between 55 and 87 during the course of administration of the drug.

Side Effects of Using Tesamorelin

Tesamorelin has been found to be potentially safe for human consumption. However, it is important to be cognizant of the mild side effects which have been observed. These side effects are as follows:
Redness, swelling, or irritation at the site of injection.
Muscle pain
Nausea or vomiting
Sweating
Mild itchiness

The peptide might have cross-reactivity with certain drugs. Hence medical consultation is crucial before the use of the molecule. Cholesterol medications such as Zocor and HIV-antiretroviral drugs such as Norvir can show adverse effects when used with the drug.

Other Things to Consider

Tesamorelin cannot be used by pregnant women or by those who are planning to conceive. Visceral fat is required for pregnancy. The drug promotes fat metabolism and thus is unsuitable during pregnancy. Medical consultation is also recommended for use of the molecule for diabetic patients. It increases the levels of insulin growth factor 1 (IGF-1). This can lead to fluctuations in blood sugar levels. Such a situation will demand constant monitoring of blood sugar.
In a nutshell, Tesamorelin turns out to be a wonder drug for fitness enthusiasts and bodybuilders. It helps in the metabolism of difficult abdominal fat and helps to achieve fitness goals faster. By triggering the release of growth hormone, it improves the general metabolism and energy homeostasis of the body. The peptide has diverse beneficial influences such as improving cognitive capabilities with only minimal side effects. The amino acid composition and the hexanoic acid modification confers the beneficial functions to the peptide similar to growth-hormone-releasing-hormone. In fact, the short stretch of the peptide helps to overcome the adverse effects of excess full-length GHRH. However, the peptide has to be used upon medical recommendation only and is not recommended for pregnant ladies and diabetic patients.

Disclaimer: The products mentioned are not for human or animal consumption. All the information shared in this article is for educational purposes only.

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