Melanotan is a synthetic peptide that is widely studied for its possible therapeutic use in various contexts. The two types of melanotan are identified as melanotan 1 (MT-I) and melanotan 2 (MT-II), with key differences in their structures and effects. Both are commonly used as sunless tanning agents, in addition to other therapeutic applications.
Here, we will explore the similarities and differences between MT-I and MT-II, including their potential benefits, side effects, and proper use. Plus, we will name the best online source for purchasing quality research peptides.
Read on to learn how to safely and effectively handle these breakthrough peptides in your research.
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What is Melanotan 1?
Melanotan 1 (MT-I) is a synthetic analog of alpha-melanocyte-stimulating hormone (α-MSH), an organic neuropeptide that plays an important role in the body’s melanocortin system. As a melanocortin agonist, α-MSH acts upon the melanocortin receptors that regulate various physiological processes, including melanin synthesis, sexual stimulation, metabolism, and immune response .
The structure of melanotan 1 is very similar to the endogenous α-MSH neuropeptide, a linear chain of 13 amino acids. However, the fourth and seventh amino acids (methionine and L- phenylalanine, respectively) of the organic hormone are replaced with norleucine and D-phenylalanine in the synthetic analog. This affords the synthetic molecule a longer half-life and stronger stimulus of the melanocortin receptor 1 (MC1R) that regulates melanogenesis [1, 2].
In its capacity as an MC1R agonist, MT-I promotes melanin synthesis to give the skin a darkened, tanned appearance. While it was initially developed and studied as a sunless tanning and photoprotective agent, clinical research has indicated its potential in other therapeutic contexts, such as enhancing inflammatory and immune responses. It is also evidenced as a possible treatment for acute photodermatoses, including erythropoietic protoporphyria and polymorphic light eruption [1, 3, 4].
What is Melanotan 2?
Like MT-I, melanotan 2 (MT-II) is a synthetic peptide analog of alpha-melanocyte-stimulating hormone (α-MSH). As a melanocortin agonist, it too acts on the body’s melanocortin receptors, involved in sexual function, melanin synthesis, and immunological response, among other biological processes [1, 5].
Unlike the long and linear structures of MT-I and α-MSH, melanotan 2 has a short, ringed form. It is more potent than α-MSH, exhibiting a stronger effect on the various melanocortin receptors, namely MC1R and MC4R. This affords it additional potential benefits, as well as a greater range of possible side effects .
Melanotan 2 acts primarily on melanocortin receptors 1 and 4 (MC1R and MC4R), which respectively regulate melanogenesis and sexual behavior. It also exhibits some interaction at MC3R, linked with metabolic processes. Like MT-I, it was first developed as a tanning agent. Ongoing analysis has suggested additional clinical applications, such as combating erectile dysfunction in men, addiction, and obesity [1, 5].
A related yet highly modified α-MSH derivative called PT-141 is similarly used in clinical settings, and is approved as a treatment of low libido in premenopausal women [4, 6].
Read on to learn more about the potential benefits of both MT-I and MT-II, as well as how to properly handle these cutting-edge peptides. Plus, you will discover where to source the highest-grade research products online!
Melanotan 1 Benefits
Clinical research has uncovered numerous possible benefits of properly administered melanotan 1. These are the primary potential benefits:
The primary application of MT-I is to increase the rate of tanning in response to UV-B light, reducing sunburned cells with a photoprotective effect. It is a powerful agonist of the melanocortin 1 receptor, which regulates melanin synthesis [1, 2, 4].
Neuroprotection and Cognitive Enhancement
In clinical trials, MT-I has been shown to improve the mental health of patients undergoing photodynamic therapy for cancer treatment. Animal studies indicate that MT-I also protects against cognitive decline due to Alzheimer’s disease and stroke [7, 8].
Treatment of Acute Dermatoses
The photoprotective effects of MT-I are beneficial for those with photosensitivity disorders. It was approved by the United States Food and Drug Administration in 2019 as a treatment for erythropoietic protoporphyria. It is under analysis for its potential to treat solar dermatitis, xeroderma pigmentosum, and polymorphic light eruption [1, 9, 10].
Melanotan 1 has also shown promise in clinical trials as an acne treatment and anti-inflammatory agent. Additional potential benefits include enhanced cardiovascular health, sexual function, and body composition [4, 11, 12, 13, 14].
Melanotan 2 Benefits
Research indicates these primary benefits of melanotan 2:
Melanogenesis for a Tanning Effect
Like MT-I, MT-II also has melanotropic effects, stimulating melanin synthesis through the MC1R receptor to visibly darken skin tone. Higher melanin levels also have photoprotective benefits, possibly reducing the risk of skin cancer and photodamage due to UV exposure [4, 15].
Melanotan 2 stimulates the melanocortin receptors 3 and 4 to regulate sexual response in both females and males. Its potency as a treatment of erectile dysfunction in male subjects is especially notable [5, 16, 17].
Treating Behavioral Disorders and Addiction
Animal studies indicate that MT-II upregulates oxytocin through MC4R stimulation to reduce autistic behaviors such as lack of social attunement and difficulty with communication. It may also combat addictive and impulsive behaviors through the hypothalamic effects of MC4R stimulation [18, 19].
In animal studies, MC4R activation has also been shown to reduce appetite and modify macronutrient preferences to reduce sugar and fat consumption. In this capacity, MT-II is being studied as a potential treatment for obesity .
By targeting MC3R and MC4R, melanotan 2 has been shown to regulate blood sugar, with some researchers viewing it as a potential treatment of metabolic disease .
Clinical research ties MT-II to reduced adiposity in animal subjects, as the melanocortin system regulates fat storage and energy expenditure, contributing to its ongoing study as an obesity treatment .
Like MT-I, melanonan 2 is currently under review for emerging benefits in addition to these.
Melanotan 1 Side Effects
Now that we have explored the many benefits of melanotan, let’s take a look at the possible side effects. Melanotan 1 has a favorable safety profile, displaying few significant side effects in clinical trials.
Studies on the long-term effects of melanotan are lacking due to the relatively recent development of therapeutic formulations. Thus, research on the lasting effects of MT-I is ongoing, pending further data.
The most commonly noted transient adverse effects in clinical trials include the following :
- Facial flushing
Rare possible side effects include [23, 24, 25]:
- Irritation at the site of administration
- Melanocytic nevus
Some of the above side effects pertain only to subcutaneous MT-I implants as reviewed in clinical trials. Specialists caution against the use of MT-I and MT-II in patients with body dysmorphia, particularly relating to skin tone. In the majority of cases, notable side effects resolve with the suspension of treatment.
The incidence of side effects often corresponds with low-quality peptides sourced from questionable suppliers, as well as failure to comply with dosage guidelines. Impure MT-I products may contain contaminants that are linked to systemic toxicity. Researchers are therefore advised to purchase peptides from trusted sources and adhere to standard dosage guidelines .
Melanotan 2 Side Effects
Several possible side effects of melanotan 2 have also been evidenced in clinical trials. As with MT-I, there is currently no available research on the long-term effects of MT-II. Here, we will explore the main clinical findings on the immediate potential side effects of melanotan 2.
A study on three male subjects in good health who received subcutaneous melanotan 2 injections daily in doses of 0.01mg/kg displayed these side effects during a two-week trial :
- Spontaneous erections
In clinical trials, the administration of MT-II has been linked with the development of naevi (moles) or the darkening of extant ones. Additional minor side effects have been observed, such as :
- Facial flushing
- Patchy skin pigmentation
- Streaks of pigmentation in the nails
- Changes in sense of taste
Acute side effects are rare and can include :
- Heart palpitations
- Abdominal pain
As noted with MT-I, the use of MT-II is not recommended in individuals presenting symptoms of body dysmorphia. In most cases, unwanted side effects disappear with cessation of use and are aggravated by variables such as tanning bed use, drug interactions, and comorbidities.
Researchers are advised to source melanotan 2 from strictly reputable suppliers.
Melanotan 1 Dosage Guide
Now, let’s explore the recommended dosage of melanotan 1. Outside of its FDA-approved use as an EPP treatment, there is no standard dosage to date. However, research suggests the following dosage guidelines for the administration of melanotan 1 [26, 27, 28]:
- When administered through subcutaneous injection, therapeutic doses start from 1mg per day.
- It is advisable to start with a low dose and increase it as needed.
- Clinical trials on the use of melanotan 1 as a tanning agent have applied daily injectable doses from 0.08 mg/kg to 0.16 mg/kg for up to four weeks.
- When used to promote tanning of the skin, MT-I injections are typically paired with scheduled UV exposure.
- Some studies on the use of melanotan 1 to treat symptoms of erectile dysfunction indicate a therapeutic baseline of 0.025 mg/kg daily.
- In clinical trials, the schedules of administration as well as the trial lengths are variable. Long-term studies are pending.
In its FDA-approved use as a prescribed treatment for phototoxicity due to erythropoietic protoporphyria (EPP), melanotan 1 is administered as a subcutaneous implant. A single implant contains 16mg and is left in place for two months .
Melanotan 2 Dosage Guide
Melanotan 2 has not been approved by the FDA, so formal dosage guidelines are pending . However, researchers have settled on certain recommendations in clinical studies. These include the following findings :
- When MT-II is injected subcutaneously, the baseline therapeutic dose is 500mcg per day.
- Experts advise that it is best to begin with a low dose and increase it incrementally to the standard daily dose.
- This dose is shown to be optimal for obtaining desired results with minimal side effects. However, the target dose may vary with the therapeutic context.
- A daily dose of 1mg/kg has not been exceeded in clinical trials.
- Schedules of administration are changeable, ranging from one to more weeks. It is not recommended to use MT-II indefinitely.
- When applied as a tanning agent, MT-II is generally injected before scheduled windows of UV exposure. Tanning times do not exceed 60 minutes.
To reconstitute either melanotan 1 or 2 before injection, the following materials are required:
- Vial of bacteriostatic water
- Vial of lyophilized MT-I or MT-II
- Alcohol wipes
- Sterile syringe
The reconstitution process is as follows:
- Wipe down all materials with alcohol swabs to reduce the risk of contamination.
- Thrust the syringe into the bacteriostatic water vial and draw out a small amount, usually no more than 2ml, depending on the dosage.
- Gradually introduce the bacteriostatic water into the vial of peptide powder, allowing it to slowly dissolve the powder.
- Refrain from shaking or stirring the vial, as doing so can damage the contents. When properly reconstituted, the solution will appear to be clear.
- Any unused solution may be refrigerated for future use.
Melanotan 1 vs. Melanotan 2 | The Biggest Differences
While melanotan 1 and 2 have many shared qualities, there are several significant differences between them. Researchers handling both types of melanotan should be aware of these points of contrast between the two:
Structure [1, 30, 31]
Although both are synthetic analogs of alpha-melanocyte-stimulating hormone (α-MSH), an endogenous melanocortin agonist, melanotan 1 and 2 are structurally distinct molecules.
- Melanotan 1 ([Nle4-D-Phe7]-α-MSH): Like α-MSH, melanotan 1 is classed as a linear tridecapeptide, consisting of an elongated chain of 13 amino acids. More potent than its parent hormone, melanotan 1 replaces the fourth and seventh amino acids of α-MSH, methionine and L-phenylalanine, with norleucine and D-phenylalanine respectively.
- Melanotan 2 (Ac-Nle-[Asp-His-D-Phe-Arg-Trp-Lys]- α-MSH-NH2): In contrast to the linear structure of melanotan 1 and α-MSH, melanotan 2 is classed as a cyclic heptapeptide. It displays a ringed form and is a substantially more modified derivative of α-MSH.
Biological Function [1, 2, 4, 5]
Due to their distinct structures, melanotan 1 and 2 interact differently with the body’s five melanocortin receptors, eliciting varying physiological responses. Although both are relatively non-specific melanocortin agonists, they display greater activity on certain receptors.
- Melanotan 1 binds primarily with MC1R, which regulates melanogenesis.
- Melanotan 2 binds with MC1R, as well as MC3R and MC4R, respectively linked with metabolic and sexual processes.
Potential Therapeutic Applications [1, 4, 5]
Their differing biological mechanisms lead to varying therapeutic applications.
- Melanotan 1 has greater affinity at MC1R and thus elicits a stronger tanning effect with fewer secondary reactions. This accounts for its principal therapeutic use as a tanning agent and treatment for photosensitivity disorders. It is under study for additional benefits, such as neuroprotective and anti-inflammatory effects, as well as cardiovascular health.
- Melanotan 2 also interacts with MC1R and is applied as a tanning agent. However, its affinity at MC3R and MC4R lends it the therapeutic potential to treat sexual dysfunction such as ED, behavioral disorders, and obesity. Specific behavioral contexts include autism spectrum disorders and addiction. As an obesity treatment, it has been noted to potentially suppress appetite, regulate blood sugar, and reduce body fat.
Side Effects [2, 4, 15, 23]
These two peptides exhibit different side effects.
- In general, melanotan 1 has presented fewer and less severe side effects in clinical studies. These include facial flushing, dizziness, fatigue, and melanocytic nevus.
- Melanotan 2 has exhibited a wider range of side effects. Mild ones include repeated yawning and stretching, spontaneous erections, and uneven skin pigmentation. More severe side effects such as seizures, priapism, and melanoma are rare but in evidence.
Administration [15, 23, 26]
Researchers have established different dosage and administration practices for melanotan 1 and 2.
- Notably, melanotan 1 has been approved by the FDA for use as a subcutaneous implant, while melanotan 2 has not.
- When administered via subcutaneous injection, therapeutic doses of melanotan 1 range from 1 mg per day to 2 mg per day.
- Daily injected doses of melanotan 2 range from 250mcg to 1 mg, with a standard dose of 500mcg per day.
- Depending on the desired therapeutic outcomes, duration and frequency of use are also subject to change.
Pharmacological Research and Development [2, 6]
Perhaps unsurprisingly, the clinical research and product development of melanotan 1 and melanotan 2 have historically differed. To briefly summarize:
- Melanotan 1 was initially developed in the 1980s as a sunless tanning agent. It has since been approved by the FDA under the generic title afamelanotide to treat erythropoietic protoporphyria, administered via subcutaneous injection.
- Melanotan 2 has been more closely studied for its potential to treat sexual dysfunction. Researchers have also developed an MT-II analog called PT-141, now a mainstay treatment of hypoactive sexual dysfunction disorder (HSDD) in premenopausal women.
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Bacteriostatic Water for Injection
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Melanotan 1 vs. Melanotan 2 | Verdict
In their function as melanocortin agonists, melanotan 1 and melanotan 2 exhibit great potential in a range of therapeutic contexts.
When it comes to choosing between the two, researchers are encouraged to consider their unique cases. While melanotan 1 may be more appropriate for a desired melanogenic outcome, melanotan 2 is perhaps more applicable to cases of sexual dysfunction. Additional benefits of each are unfolding with emerging research and innovation.
We hope you have enjoyed this in-depth exploration of the data to date and come to the conclusion that neither peptide is bar-none better than the other. The use of each is highly dependent on the research context, and handlers must proceed accordingly.
Whichever peptide you choose, be sure to purchase it from a trusted source and adhere to the guidelines and precautions put forth by experts. Both peptides surely have exciting futures in a range of clinical settings, making dynamic additions to your research toolkit.