GMP Melanotan I Legit Peptide Hormones CAS 121062-08-6 For Skin Tanning

Quick Information

Introduction

Melanotan I is a cyclic heptapeptide analog of the alpha-melanocyte stimulating hormone (a-MSH) that tends to induce skin tanning. Melanotan II has the additional effect of increasing libido.

Researchers there knew that one of the best defenses against skin cancer was a natural tan which has been slowly developed over weeks. They hypothesized that an effective way to reduce skin cancer rates in people would be to induce the body's natural tanning system to produce a protective tan prior to UV exposure. They knew the body's naturally occurring hormone alpha-melanocyte stimulating hormone (α-MSH) caused melanogenesis, a process by which the skin's tanning cells (melanocytes) produce the skin's tanning pigment (melanin). With that knowledge they tested to see if administering this hormone to the body directly could be an effective method to cause sunless tanning. What they found was that while it appeared to work, natural alpha-MSH had too short a half life in the body to be practical as a therapeutic drug. So they decided to find a more potent and stable alternative, one that would be more practical.

After synthesizing and screening hundreds of molecules, the researchers headed by Dr. Victor Hruby, found a peptide that after trials and testing seemed to not only be safe but also approximately 1,000 times more potent than natural α-MSH. They dubbed this new peptide Melanotan. Since their discovery, numerous studies dating back to the mid-1980s have shown no obvious toxic effects of Melanotan. Because skin cancer (melanoma) today is a major health concern, Melanotan is expected to be used as a drug to combat it. Melanotan will do this by stimulating the body's natural tanning mechanism to create a tan without first needing exposure to harmful levels of UV radiation. This in turn will reduce the potential for skin damage that can eventually lead to skin cancer.

The Development of Melanotan 1

The initial creation of the Melanotan 1 peptide tanning analogue can be credited to the University of Arizona. During the course of study aimed at developing a defense against skin cancer, focus was placed on developing a method of stimulating natural melanogenesis, or the natural production of melanin in the skin, without direct exposure to the potentially harmful ultraviolet radiation in sunlight. Initially, University of Arizona researchers attempted to directly administer the naturally occurring hormone alpha-MSH in order to elicit this desired result.

Although this strategy exhibited promising results, it was determined that the naturally occurring MSH had a prohibitively short half-life to be of realistic use as a therapeutic remedy. However, the positive results gleaned from MSH administration encouraged further research into the development of Melanotan-1, which exhibits similar effects whilst possessing an extended half-life for functional therapeutic utilization. The researchers, headed by Victor J. Hruby and Mac E. Hadley, found a peptide, [Nle4, D-Phe7]-α-MSH, that was approximately 1,000 times more potent than natural α-MSH. They named this new peptide molecule "Melanotan" (later Melanotan-1).

Application

Melanotan produces its photoprotective effects by triggering a 'signaling cascade' via its activation of the MC1R on melanin-producing cells known as melanocytes. Upon Melanotan binding with the MC1R on the surface of melanocytes in the epidermal layer of the skin, it begins a series of actions and reactions that result in melanocytes favoring the production of eumelanin (photoprotective black/brown pigment). The initial binding activates the MC1R leading to the activation of adenylate cyclase (AC) and stimulation of the production of cyclic adenosine monophosphate (cAMP).

A (PKA) resulting in the phosphorylation of the cAMP response element-binding (CREB). Phosphorylated CREB will bind to the cAMP response element (CRE) on the microphthalmia-associated transcription factor (MITF) gene leading to the synthesis of the MITF protein. MITF has the ability to activate several genes by binding to them, including the MC1R gene and the genes involved in melanogenesis. This results in increased concentrations of the melanogenic enzymes within the melanocyte.

Description
1.MT-1 (or Melanotan I,or Afamelanotide,or CUV-1647) is a synthetic analog of peptides nature of endogenous melanocortine peptide alpha-melanocyte stimulating hormone.It has hormones nature as well as common proteins features,its molecular weight/mass is 1646.88 and its molecular formula is C78H111N21O19.

2.Afamelanotide was specifically developed by American scientists LED by V.Hruby in 1991 as a possible research compound that can be used against skin cancer by stimulating tanning system which in own turn would generate protective natural tan during melanogenesis.So that synthetic analog was created to determine if it can show the same effect and stimulate melanocytes to produce and release melanin to protect skin from UV.Most of studies and trials were conducted in United States and Australia.

3.Developed research compound is quite stable cyclic form of original hormone but specifically has much longer half-life period.It works as agonist of specific melanocortin receptor and possesses such property as being selective;And thus it promotes increased level of eumelanin above usual pheomelanin,which provides higher efficacy of photoprotection abilities.

MT-1 (Melanotan I) Effect:

1. Melanotan 1 is an analogue of MSH, which is manufactured within the pituitary gland. It is classified as a melanocortin, and, like all melanocortins, it acts on certain physical systems which influence hair color, skin pigment, sexual arousal, sexual desire and appetite.

2. The more melanin the body produces, the darker the skin gets. This peptide will allow for self-tanning without UV exposure. This means that the body will grow tanned all over, even in places which aren't exposed to sunlight.

3. However, UV exposure will accelerate the tanning process in exposed areas. The role that UV exposure plays sometimes results in a tan which may not be perfectly even all over.

4. Most users find that they are most tanned on their faces, arms and stomachs. The genitals may also take on a tanned appearance during therapy with this peptide.

Usage

Melanotan 1 (also referred to as Afamelanotide) is a synthetic peptide variant of a peptide hormone, called alpha-Melanocyte stimulating hormone or MSH that is naturally produced in the body and is responsible for stimulating melanogenesis, a peptide process for pigmentation of the skin. Alpha-MSH activates certain melanocortin receptors in the process of exerting its effects. Indeed, MSH also exerts potent influence over lipid metabolism, appetite, and sexual libido via these melanocortin receptors. As a result, Melanotan-1 sunless skin tanning effects. While Melanotan 2 and PT-141 have been studied at length as a potential remedies for the treatment of sexual dysfunction, Melanotan-1 has been researched extensively for use in protecting against the harmful effects of ultraviolet radiation from sunlight due to its melanogenesis-stimulating properties.

Both Melanotan-1 and Melanotan 2 are analogs of the peptide hormone alpha-melanocyte stimulating hormone (α -MSH) that tend to induce skin tanning. Unlike Melanotan 1, Melanotan 2 has been shown to have aphrodisiac properties, the additional effect of increasing libido. Melanotan-1 is a non selective agonist of the melanocortin receptors (MC1R, MC3-5R). As an analogue of α -MSH, its mechanism of action is biomimicry of the natural mammalian tanning process.