What Are Peptides? Uses, Side Effects, and Clinical Data

Curious about therapeutic peptides?

Peptides are among today’s most promising innovations in health and wellness.

Inside this in-depth guide, we detail exactly what you must know about this exciting new field of clinical research, including…

• What are peptides?

• Peptide uses and benefits

• Peptides for targeted effects

• Peptide dosage guide

• Peptide safety and legality

… and more!

At Peptides.org, we specialize in bringing you the most up-to-date research peptide information and clinical data, so you can be assured that all content provided has been sourced and vetted by experts.

To set you up for success, we will also give you our highest recommendation for buying superior research peptides online.

What Are Peptides? | A-Z Guide

Peptides are molecules made of amino acid residue chains that are joined in covalent bonds. This broad molecular class comprises an estimated 13,000 naturally occurring peptides and approximately 1 × 1013 synthetic ones [1, 2].

Structure

Peptides are classed according to their structure (cyclic or linear), length, and molecular weight, which determines their oral bioavailability. Typically defined as chains of 2-50 amino acid residues, peptide subclasses include oligopeptides of roughly 10-20 amino acids and polypeptides of about 20-50 amino acids. Polypeptides are the building blocks of proteins. These categories are somewhat flexible and overlapping [2, 3].

Research and Development

Peptide therapy entails the administration of synthetic or modified organic peptides in clinical contexts. Ongoing studies have seen the development of peptide therapeutics, which are medical preparations of bioactive peptides that have been augmented to provide enhanced bioavailability, more targeted effects, and longer half-lives. Peptide therapeutics can be incorporated into peptide-based drugs, optimizing the specificity and efficacy of peroral, small-molecule medications [1, 2, 3].

Endogenous peptides regulate many vital physiological processes, functioning variously as neurotransmitters, hormones, growth factors, and other key biochemical actors. Peptide therapeutics include synthetic analogs of endogenous peptides as well as peptides that mimic endogenous substances for targeted effects [2, 4].

Peptide research began in the early 20th century with the study of natural hormones such as oxytocin, insulin, and vasopressin. Insulin is considered to be the first therapeutic peptide, isolated from a natural source in 1921 and shortly developed into a commercial peptide drug for the treatment of diabetes. Since then, evolving technology has seen the development of synthetic peptidyl analogs to endogenous peptides such as oxytocin, vasopressin, growth hormone-releasing hormone, and many more [4].

Read on to learn more about the specific applications of therapeutic peptides, including their safety, legality, and unique advantages in a range of therapeutic contexts.

What are Peptides Used For?

Peptides have evidenced therapeutic benefits in an impressive array of contexts. Peptides and peptide-based drugs have been approved as treatments and diagnostic tools in areas such as oncology, endocrinology, dermatology, sexual health, and cardiometabolic conditions [5].

Due to the novelty of the field, a vast number of therapeutic peptides have yet to receive regulatory approval for medical use. However, research indicates the potential of peptides in numerous areas of clinical interest. These include:

Wound and Injury Recovery

Peptides such as BPC-157 and TB-500 are shown to accelerate and improve the healing process of different tissue types, including muscle, bone, skin, and tendons. This is achieved through several biological mechanisms, such as the promotion of angiogenesis, the activation of growth factors, and broad anti-inflammatory effects [6, 7].

Muscle Growth

Growth hormone secretagogues like ipamorelin and sermorelin are evidenced to stimulate muscle, bone, and blood vessel growth, boosting overall lean muscle mass [8, 9].

Fat Loss

Peptides such as the growth hormone secretagogue tesamorelin and growth hormone fragment frag 176-191 show targeted metabolic effects linked to body fat reduction and weight loss [10, 11].

Anti-aging

Some peptides show potent anti-aging and protective outcomes. For example, epithalon promotes cellular regeneration through telomere upregulation and antioxidant activity, addressing age-related disorders like cognitive decline, cancer, and inflammatory disease [12].

Sexual Health

Studies show that peptides such as PT-141 and melanotan 2 act upon the body’s melanocortin system to boost sexual arousal and counter sexual dysfunction in both male and female subjects [13, 14].

Skincare

Regenerative peptides like GHK-Cu have been shown to promote the production of collagen to visibly improve skin elasticity, tone, and firmness [15].

Peptides have many more clinical applications beyond the scope of this article.

Benefits of Peptides

Peptides offer unique advantages over other therapeutic and pharmaceutical compounds. They are prized for their safety, targeted effects, and synergistic biological activity, wedding the specificity and tolerability of small molecule drugs with the low immunogenicity and cost-effectiveness of larger biologics [16].

Both synthetic and natural peptides show therapeutic promise in many contexts, from neurological and sexual health to improved body composition and physical performance. Their evidenced benefits are steadily increasing with advances in methods of peptide synthesis that optimize their potency, half-life, and bioavailability.

For example, cutting-edge oral preparations of BPC-157 and TB-500 have recently become available, enhancing their cytoprotective effects. Many peptides are under close investigation for their utility in vaccines and diagnostics, and most are pleiotropic compounds, eliciting benefits beyond their primary intended applications [4, 17].

Read on to discover the best peptides for specific clinical targets.

Peptides For Skincare

Peptides are making a splash in the field of skincare, with GHK-Cu, Argireline, and Vilon being among the most heavily researched.

GHK-Cu

This tripeptide is linked with numerous skin benefits attributed to its copper-binding ability. GHK-Cu is natural to human plasma and its levels decline with age. It is shown to promote skin cell renewal and wound healing, stimulating the production of collagen and blood vessel formation while combating oxidative stress. Further, GHK-Cu is evidenced to promote dermal stem cell proliferation and migration to heal and fortify the skin matrix.

The action of GHK-Cu visibly improves skin quality in terms of elasticity, firmness, tone, and density, especially in subjects of advanced age. This peptide is also observed to be beneficial in dermal transplants and scar reduction. In studies, GHK-Cu has been applied in topical creams and via injection [15].

Argireline

Also known as acetyl hexapeptide-3, Argireline is noted for its enduring anti-wrinkle effects on the skin. Composed of six amino acids, it is commercially available in topical skincare formulations. Argireline is evidenced to inhibit neurotransmitter release, decreasing facial muscle activity to prevent wrinkle formation.

It is considered a safer and less invasive alternative to botox injections and has demonstrated comparable efficacy in reducing visible fine lines and wrinkles. Studies on its topical use have also shown it to boost skin hydration, firmness, and elasticity with visibly rejuvenating effects [18].

Vilon

Alternately known as Lys-Gly or lysylglutamic acid, Vilon is a synthetic dipeptide with demonstrated bioregulatory, immunomodulatory, and anti-aging effects. Made of only two amino acids, it is of growing interest in anti-aging research. It is shown to stimulate tissue regeneration, enhancing endothelial and immune function. It has also been shown to increase collagen production and fibroblast proliferation, thereby enhancing connective tissue health.

These mechanisms of Vilon may combine to prevent and reverse visible signs of skin aging such as wrinkles, discoloration, and scarring. The peptide’s regenerative effects show clinical potential in many additional areas, from the treatment of cancer to metabolic disease [19, 20].

Peptides For Weight Loss

With roughly two out of three adults in the United States being overweight or obese, peptides for weight loss is as critical an application as ever. Research in this area includes compounds like tirzepatide, tesamorelin, and HGH fragment 176-191.

Tirzepatide

Approved by the US FDA for the treatment of type 2 diabetes, tirzepatide is a synthetic analog of the human gastric-inhibitory polypeptide (GIP), which is a key regulator of metabolic processes and appetite. The linear peptide of 39 amino acids has been shown to affect glycemic control through dual activity on two distinct incretin receptors, GIP and GLP-1, affording it the potential to treat both diabetes and obesity.

It has been linked with weight loss, reduced adiposity, and overall improved body composition in subjects with cardiovascular disease. Similarly, tirzepatide was shown to improve glucose response in healthy subjects over a 4-week trial period [21].

Learn more about the Tirzepatide peptide here.

Tesamorelin

Tesamorelin is a 44-amino acid peptide is a synthetic analog of the human growth hormone-releasing hormone (GHRH), working to stimulate the release of endogenous growth hormone (hGH). Also known as tesamorelin acetate, it shows greater stability and potency than endogenous GHRH and is an FDA-approved treatment for excessive abdominal adiposity in HIV patients with lipodystrophy.

It is evidenced to boost metabolic health through improved insulin resistance and cholesterol levels. In reducing visceral adiposity, it may also reduce cardiovascular risk in vulnerable populations. Tesamorelin has a favorable safety profile as evidenced in clinical trials [10].

Frag 176-191

A synthetic peptide fragment of human growth hormone, frag 176-191 is a GH receptor agonist whose noted benefits mirror those of its parent hormone. Studies suggest that it boosts thermogenesis and promotes weight loss as well as cartilage repair. Its blood sugar-regulating effects indicate its potential as a diabetes treatment, pending further analysis.

In one animal study, a single dose of frag 176-191 delivered via intravenous injection dramatically reduced insulin sensitivity. Another study showed it to reduce weight and body fat in obese mice over a 14-day period. Relatively under-studied, frag 176-191 requires more analysis to confirm these promising potential benefits in humans [11, 22].

Peptides For Bodybuilding

A number of peptides, including ipamorelin and sermorelin, as well as the nonpeptide GHS MK-677 are actively studied for their abilities to improve body composition and muscle function in test subjects.

Ipamorelin

A synthetic pentapeptide and ghrelin mimetic, ipamorelin selectively triggers the release of human growth hormone (hGH) within the pituitary gland. It was derived from GHRP-1 and is known as the first peptidyl GH secretagogue to achieve selective GH release. Growth hormone secretagogues are shown to increase lean muscle mass with anabolic effects while improving quality of sleep.

Animal studies indicate the ability of ipamorelin to attenuate muscle catabolism due to glucocorticoid use while promoting the growth of bone, capillary, and muscle tissues. It may also stimulate chondrogenesis (cartilage regeneration) to affect better joint and connective tissue health [8, 23].

Learn more about the Ipamorelin peptide here.

Sermorelin

Sermorelin, alternatively known as sermorelin acetate, is a synthetic growth hormone secretagogue that held FDA approval until 2008 as a treatment for both idiopathic and acquired growth hormone deficiency, withdrawn for reasons unrelated to performance or safety. Analogous to the human growth hormone-releasing hormone, sermorelin is composed of 29 amino acids, slightly smaller than its parent hormone for increased stability and bioavailability.

In studies on animal and human subjects, it has shown the potential to increase lean muscle mass while boosting cardiovascular health and reducing visible signs of aging. It is also under analysis for the treatment of hypogonadism in male subjects. Having undergone thorough safety trials for FDA approval, it is noted for its tolerability and low incidence of adverse effects [9].

MK-677

Also called ibutamoren, MK-677 is a nonpeptide growth hormone secretagogue and synthetic ghrelin agonist, prized for its high oral bioavailability and targeted effects on the GH/IGF-1 axis. It has been studied as a treatment for growth hormone deficiency and shown to positively impact physical composition in healthy subjects, as well.

Although it functionally compares to GHRP-6, MK-677 is classed as a peptide mimetic, more stable than peptidyl structures. Its targeted GH release is evidenced to boost the growth of many tissue types and combat diet-induced catabolism [8, 24].

Peptides For Healing

BPC-157 and TB-500 lead the pack of peptides prized for their efficacy in injury recovery and wound healing contexts.

BPC-157

Body protection compound-157, also called BPC-157, is a synthetic derivative of the endogenous gastro peptide called body protection compound, natural to human digestive fluid. The pentadecapeptide stimulates blood vessel formation, a process known as angiogenesis, to protect and fortify the gastrointestinal lining and promote healthy GI function.

It is also shown to boost cellular renewal in various organ systems and has strong anti-inflammatory effects. The benefits of BPC-157 have been noted in multiple tissue types, including the bones, cardiovascular system, tendons, ligaments, and skin. Through the gut-brain axis, it may also have neuroprotective effects. Studies further indicate its antidote properties against multiple drug toxicities, such as NSAIDs, alcohol, and insulin. Available in both parenteral and oral formulations, BPC-157 has a positive safety profile to date [6, 17].

TB-500

TB-500 is a synthetic analog of thymosin-beta 4 (TB4), a regenerative peptide found in most animal and human cells. The 43 amino acid peptide promotes cellular migration and upregulates vascular endothelial growth factor (VEGF) to boost angiogenesis, central to wound healing and injury recovery. Released by macrophages and platelets after injury, it reduces inflammation, apoptosis, and the risk of infection.

TB-500 is functionally equivalent to its parent compound, evidenced to promote healing in many tissue types including cardiac, muscle, skin, corneal, and nerve cells. In topical preparations, it is shown to effectively treat chronic dermal lesions. Studies in animals suggest its potential to promote neurovascular recovery in subjects with traumatic brain and spinal injuries. It has a favorable safety profile and is available in various administration formats, including injectable, oral, and nasal [7].

Peptides For Sexual Health

The peptides PT-141 and melanotan 2, which are closely related molecules, are paving the way for peptide therapy in the field of sexual health.

PT-141

Assigned the generic name bremelanotide, PT-141 is a synthetic melanocortin agonist and derivative of alpha-melanocyte-stimulating hormone (α-MSH). It stimulates the melanocortin receptors to boost sexual health in both sexes. PT-141 shows an affinity for melanocortin receptor 4, which has a powerful modulatory effect on sexual function and arousal.

Its effects on sexual arousal may also be achieved through the stimulation of dopamine release within the hypothalamus. This cyclic heptapeptide is FDA-approved for the treatment of hyposexuality in premenopausal women. It is also under analysis as a potential treatment for male erectile dysfunction, as well [13, 25].

Melanotan 2

A synthetic analog of alpha-melanocyte-stimulating hormone (α-MSH), melanotan 2 (MT-II) is a melanocortin agonist that shows a high affinity for melanocortin receptors 1 and 4. These respectively modulate dermal melanin production and sexual arousal. MT-II is a cyclic heptapeptide, structurally distinct from endogenous α-MSH, which is larger and linear. Its modified form increases its potency and specificity.

While it was initially developed as a sunless tanning agent due to its melanotropic effects, it has been shown to enhance the libido in male and female subjects with particular promise in the treatment of male erectile dysfunction. Further areas of clinical interest include the treatment of behavioral disorders, addiction, and obesity [14].

Peptides For Anti-Aging

While the anti-aging space is rife with supplement products of questionable efficacy, injectable compounds like epithalon and l-glutathione may hold the key to longevity medicine.

Epithalon

A synthetic tetrapeptide, epithalon is shown to have broad anti-aging benefits. It is functionally comparable to the endogenous pineal peptide epathalamin, a potent bioregulator that decreases stress and acts as a powerful antioxidant. While upregulating telomere activity, epithalon promotes cellular renewal and fights inflammation. Its geroprotective and longevity-boosting effects include the treatment of age-related pathologies such as cognitive decline, endocrine disorders, inflammatory diseases, and cancer.

Epithalon has been shown in long-term clinical trials to decrease overall mortality rates with particular decreases in markers of cardiovascular aging. Additional noted benefits include tumor suppression and increased melatonin output for enhanced sleep. Epithalon is further linked with improved metabolic health through increasing insulin sensitivity and normalizing cholesterol levels [12].

L-Glutathione

This synthetic tripeptide is the active form of glutathione, a potent antioxidant compound that is natural to most animal and human cells. Glutathione is essential to many physiological processes, including immune and inflammatory responses, metabolism, gene expression, mitochondrial function, and cellular proliferation. Levels of this crucial molecule naturally decline with age, a process linked with visible aging of the skin and increased risk of age-related pathogenesis.

Supplementation with exogenous L-glutathione is demonstrated to have anti-aging effects, such as reduced dermal hyperpigmentation and wrinkles with increased elasticity and hydration. Its powerful anti-inflammatory effects may also reduce the risk of numerous illnesses, including cancer, neurodegenerative conditions, cardiovascular disease, and diabetes [26, 27].

Research Peptides Side Effects

Due to the novelty of the field, most therapeutic peptides have not been extensively screened for safe use in humans and are approved strictly for use in research contexts. Handlers are therefore urged to reference all relevant studies and peer-reviewed literature before adding peptides to their experimentation.

Nonetheless, most research peptides evidence favorable safety profiles in clinical studies to date. In comparison with popular pharmaceuticals, peptide-based drugs are positively regarded for their low levels of toxicity and good tolerability in diverse populations.

As the field evolves, leading clinicians are constantly improving methods of production and safe administration. For example, top scientists have newly discovered an advanced technique for evaluating peptide toxicity, entailing digital modeling and precise results. This forecasts further increases in peptide safety [28].

Some peptides have been more heavily researched than others, and some have been thoroughly evaluated and approved by the US Food and Drug Administration (FDA) for certain uses.

For example, sermorelin held FDA approval until 2008 as a treatment and diagnostic tool for growth hormone deficiency. As such, it was subject to full safety evaluation per federal guidelines and is considered to be well-tolerated in both adults and children with correct dosage and handling. Side effects were transient and mild, including injection-site irritation and facial flushing. In rare cases, symptoms such as headache, nausea, and vomiting were noted [9, 29].

BPC-157 is another widely studied research peptide with substantial safety data. Although it has not been subject to complete FDA analysis, current findings suggest a positive safety profile. A phase 1 clinical trial for its use in treating inflammatory bowel disease evidenced good tolerability and no toxicity. Nevertheless, several minor and transient adverse reactions have been noted, namely injection site irritation, fatigue, and light-headedness [6].

Safety Measures

In most cases, side effects due to peptide administration are minor and subside with the termination or completion of the course of therapy. Adverse outcomes are associated with peptides of low quality and incorrect handling practices. Researchers are therefore advised to source all peptides from trusted retailers and comply with established protocols in preparation, administration, dosage, and storage. This requires familiarity with all relevant literature and studies on therapeutic peptides, including FDA data and peer-reviewed scientific publications. Care should be taken in safely preparing peptides for injection, including the use of sterile tools as directed by experts.

Peptides Dosage Guide

Given the diversity of research peptides, a complete dosage guide is beyond the scope of this article. When handling peptides for research purposes, scientists should refer to all relevant publications to determine the administration and dosage practices most agreed upon by experts. Some peptides may require cycled dosing schedules, and routes of administration are subject to vary. While some peptides may be topically, nasally, or orally administered, many are best suited to injection.

With these precautions in mind, qualified researchers may use our preferred peptide dosage calculator when preparing therapeutic peptides for injection.

See our Peptide Dosage Calculator to access a cutting-edge tool to properly dose injectable research peptides.

Improper dosage and administration of research peptides can lead not only to faulty findings but in some cases hazardous adverse effects. Adherence to dosage protocols is required.

Where to Buy Peptides Online?

Purchasing peptides from a legitimate retailer is key for safe and effective research. Unfortunately, the web is saturated with low-quality vendors and sub-par peptide products.

Luckily, the experts at Peptides.org have thoroughly explored the market to provide you with our absolute highest recommendation for buying superior research peptides online.

Look no further than Peptide Sciences.

This US-based retailer is the premier research peptide source for leading scientists worldwide. It is noted not only for its unsurpassed product quality and diversity but its peak business practices and track record of customer satisfaction. Let’s break down the reasons you are guaranteed to have an unbeatable experience with Peptide Sciences:

• Peptide Quality is Guaranteed: All premium peptides are produced domestically in exclusive collaboration with ISO 9001:2008 and WHO/GMP-approved manufacturers. Minimum purity levels of 99% are guaranteed and verified with valid certificates of analysis from third-party laboratories. Quality screenings include mass spectrometry (MS) and high-performance liquid chromatography (HPCL) methods of analysis, the most precise and reliable techniques available.

• Prices are Unbeatable: Domestic manufacturing allows Peptide Sciences to maintain low prices on its high-grade items. For example, a 5mg vial of sermorelin for injection is just $49.50, and a 5mg vial of BPC-157 is only $59.50. Plus, price reductions are offered on bulk orders!

• International, Low-Cost Shipping: Shipping to select international destinations is available at a low, flat rate. Most orders are dispatched within just 24 hours for arrival within 7-10 business days.

• Rapid, Safe Online Checkout: The user-friendly website brings you easy, secure checkout. All client data is protected with the latest SSL encryption technology, and many types of payment are accepted. From crypto to third-party processors and credit cards, Peptide Sciences has you covered.

• Total Commitment to Client Satisfaction: This retailer is driven by its core pledge to bring every customer 100% satisfaction. Helpful staff is available to respond to client queries within just 24 to 28 hours via email, and mistaken orders are replaced free of charge. Plus, the site offers top-notch educational material with links to trusted, cutting-edge sources on peptide research.

With all of these benefits, it is no wonder that Peptide Sciences is considered the gold standard of research peptide sales among experts across the globe!

Are Peptides Legal?

Therapeutic peptides that have received FDA approval are legal for use as medically directed. Peptides that have not received regulatory approval are legal for strictly research purposes and handling by qualified individuals. Researchers should avoid retailers who market unapproved peptides as medical products for human use, an illegal practice.

The novelty of the peptide industry unfortunately means that substantial regulatory measures have yet to be established. This in turn has seen the birth of an illicit underground peptide market, rife with questionable vendors, low-grade products, and illegal marketing tactics. Purchasing from such sources runs the risk of ineffective research and grave adverse effects due to contaminated and mislabeled products.

Even within the legal peptide arena, there is much room for improvement when it comes to quality control standards in large-scale peptide manufacturing. This climate impedes the approval of many peptide products for clinical trials and medical marketing. Nonetheless, the industry continues to grow as more legislators and practitioners catch on to the many potential benefits of these exciting compounds. Reforms are afoot to establish stricter guidelines on peptide manufacturing and the regularization of clinical trials for the market release of peptide therapeutics.

Buy from a Legitimate Source

In the meantime, researchers should exercise caution to purchase peptides from legal suppliers that meet these standards of legitimacy [30]:

1. The retailer should state that the peptides are sold only for research purposes and to be handled by qualified persons.

2. The marketing literature should include no claims as to the guaranteed benefits of peptide administration.

3. Because of the lack of quality regulations, peptide vendors should provide third-party lab test results establishing the purity of the peptides sold.

When sourced from reputable vendors and correctly handled by qualified researchers, peptides are fully legal.

Are Peptides Safe?

Researchers with an interest in peptide therapeutics should be advised that peptides are largely available strictly as research chemicals. As such, it falls upon handlers to refer to relevant literature on each peptide in developing safe experimental designs. Concerns over peptide toxicity, adverse effects, and tolerability can in most cases be addressed with a survey of pertinent clinical research findings.

Potential adverse effects should be considered on a case-by-case basis. Researchers may consult experimental data and clinical trial registries to gain insight into a peptide’s overall safety rating. Peptides such as sermorelin that have received FDA approval have been more thoroughly evaluated for side effects and tolerability in human test subjects.

Noted side effects related to peptide administration are in most cases minor and transient. Handlers can reduce the risks of adverse effects through adherence to establish guidelines on peptide preparation, administration, and storage. Further, safe use is predicated on buying from legitimate sources. In cases of severe adverse reactions, cease peptide administration and seek medical attention.

What Are Peptides? | Overall

This wraps up our in-depth review of peptides, including their primary applications, noted side effects, and current research findings.

This vast and versatile class of compounds is of growing clinical interest due to mounting evidence of the numerous therapeutic potentials of synthetic peptide administration, from muscle growth and fat loss to improved sexual health and anti-aging effects.

Researchers interested in therapeutic peptides are sure to enjoy our recommended selection of peptides for targeted outcomes. When properly sourced and handled, peptides make a great addition to studies on a diverse range of clinical topics. Whether your focus is bodybuilding, skincare, or improved wound healing, this guide has you covered.

Ensure the safety and effectiveness of your peptide research by sourcing your materials from our most highly recommended online peptide supplier, Peptide Sciences.

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