Synonym |
Alpha-MSH (5-13) |
Species |
Human |
Protein Accession |
P41135 |
Purity |
Greater than 95% as determined by SDS-PAGE |
Endotoxin Level |
Less than 1 EU/μg |
Biological Activity |
The activity is determined by its ability to induce cAMP accumulation in HEK293 cells
transfected with human MC1R. The ED50 for this effect is typically 0.2-1 μg/mL. |
Expression System |
E. coli |
Fusion Tag |
None |
Predicted Molecular Mass |
1089 Da |
Formulation |
Lyophilized from a 0.2 μm filtered solution of 20 mM PB, pH 7.4 |
Reconstitution |
It is recommended to reconstitute the lyophilized Alpha-MSH (5-13) in sterile 18 MΩ-cm H2O not
less than 100 μg/ml, which can then be further diluted to other aqueous solutions. |
Storage & Stability |
Lyophilized Alpha-MSH (5-13) although stable at room temperature for 3 weeks, should be stored
desiccated below -18°C. Upon reconstitution Alpha-MSH (5-13) should be stored at 4°C between 2-7
days and for future use below -18°C. |
FAQ
What is (Met5,Pro6,D-Phe7,D-Trp9,Phe10)-α-MSH (5-13) and what are its primary functions?
(Met5,Pro6,D-Phe7,D-Trp9,Phe10)-α-MSH (5-13) is a synthetic peptide analog derived from the
naturally occurring alpha-Melanocyte-Stimulating Hormone (α-MSH). It is a modified version of the α-MSH
peptide, emphasizing a truncated sequence that starts from the fifth to the thirteenth amino acid.
Alpha-MSH is primarily known for its role in stimulating melanocytes, the cells responsible for
producing melanin in the body. This characteristic has made α-MSH an area of interest in the study of
pigmentation and skin-related therapies. The modifications made in the synthetic version are intended to
enhance its stability and potency compared to the natural hormone.
The primary function of this
peptide analog lies in its interaction with melanocortin receptors, particularly MC1R, which are found
in various tissues, including the skin, brain, and immune cells. By binding to these receptors,
(Met5,Pro6,D-Phe7,D-Trp9,Phe10)-α-MSH (5-13) can influence several physiological processes. In
dermatological contexts, this interaction promotes melanin production, which results in increased
pigmentation and potentially offers photoprotective effects against ultraviolet (UV) radiation. This
potential protection is of significant interest because it could reduce the risk of skin damage and skin
cancers associated with UV exposure.
Beyond skin pigmentation, α-MSH peptides have been studied
for their potential anti-inflammatory properties. The peptide can modulate the immune response by
influencing cytokine production, which may help in reducing inflammation. This suggests possible
applications in treating inflammatory diseases and autoimmune disorders. Additionally, α-MSH and its
analogs have been investigated in neurological contexts due to their effect on behaviors related to
appetite, sexual function, and energy balance, mediated through the central nervous
system.
Researchers are also exploring the therapeutic possibilities of
(Met5,Pro6,D-Phe7,D-Trp9,Phe10)-α-MSH (5-13) in metabolic disorders. Modulating the melanocortin
pathways can have significant effects on the regulation of body weight, making it a candidate for
obesity treatment strategies. By influencing energy homeostasis and appetite control, this peptide may
offer benefits for individuals with metabolic syndrome or related conditions.
While many of the
applications of (Met5,Pro6,D-Phe7,D-Trp9,Phe10)-α-MSH (5-13) remain in experimental stages, its
versatile interactions with melanocortin receptors suggest a wide array of potential therapeutic uses.
However, more extensive clinical research is needed to fully understand its efficacy, safety, and
appropriate applications in humans.
How does (Met5,Pro6,D-Phe7,D-Trp9,Phe10)-α-MSH (5-13)
specifically affect skin pigmentation, and what are the implications of this effect?
The impact of
(Met5,Pro6,D-Phe7,D-Trp9,Phe10)-α-MSH (5-13) on skin pigmentation is primarily mediated through its
interaction with the melanocortin 1 receptor (MC1R), which is heavily present in melanocytes.
Melanocytes are the cells within the skin responsible for melanin production, the pigment that gives
skin its color and provides protection against UV radiation. When this peptide binds to MC1R, it
activates the receptor, leading to a cascade of intracellular events resulting in increased synthesis of
melanin. The process involves the upregulation of enzymes essential for melanin production, such as
tyrosinase. Consequently, this elevation in melanin can lead to darker skin tones or enhanced tanning,
providing a potential protective barrier against UV damage.
The implications of this increased
pigmentation are notable, both in dermatological health and therapeutic settings. From a dermatology
perspective, enhanced melanin production resulting from the peptide's activity can offer protective
advantages by absorbing and dissipating UV radiation more effectively than lighter-pigmented skin. This
implies significant potential for reducing the risks of photodamage, including DNA damage in skin cells,
which can eventually lead to skin cancers such as melanoma. Therefore, the peptide could be instrumental
in preventive skin health, particularly for individuals who are at higher risk due to their natural low
levels of melanin.
Additionally, the cosmetic and aesthetic industries might see the peptide as a
tool for individuals seeking to achieve darker skin tones without the adverse effects of excessive sun
exposure. This could lead to new formulations of tanning products or treatments designed to safely
stimulate melanin production.
However, the application of (Met5,Pro6,D-Phe7,D-Trp9,Phe10)-α-MSH
(5-13) in these contexts also raises important considerations. The peptide's effect on pigmentation must
be carefully controlled to avoid undesired outcomes like hyperpigmentation or uneven skin tone. There is
also a need to address potential long-term safety concerns associated with manipulating natural skin
pigmentation processes.
Thus, while the peptide's ability to enhance skin pigmentation holds
promising therapeutic and cosmetic potential, its real-world application must be approached cautiously,
ensuring comprehensive clinical testing and evaluation to determine optimal dosages and delivery
methods. Researchers and dermatologists must collaborate to assess the broader implications on skin
health and establish standardized guidelines to maximize benefits and minimize risks.
What
potential therapeutic applications are being explored for (Met5,Pro6,D-Phe7,D-Trp9,Phe10)-α-MSH (5-13)
beyond pigmentation?
Beyond its effects on pigmentation, (Met5,Pro6,D-Phe7,D-Trp9,Phe10)-α-MSH
(5-13) has shown potential in various therapeutic applications due to its interaction with melanocortin
receptors that extend beyond the skin. One significant area of interest is its anti-inflammatory
properties. The peptide's influence on the melanocortin system involves modulation of immune responses,
which can result in altered cytokine production. This action suggests potential in conditions
characterized by chronic inflammation, such as autoimmune diseases. By mitigating inflammatory
responses, the peptide could contribute to therapeutic strategies aimed at reducing disease activity and
improving patient outcomes in conditions like rheumatoid arthritis, psoriasis, and inflammatory bowel
disease.
In the realm of neurology, the peptide's ability to cross the blood-brain barrier and
influence neuronal activity opens avenues for treating neurodegenerative diseases and neurological
disorders. Research has indicated that the peptide might affect behaviors and functions related to
appetite, energy homeostasis, and sexual behaviors, which are regulated by the central nervous system.
This aspect makes it a candidate for interventions in obesity and related metabolic disorders. By
modulating the pathways involved in appetite regulation, the peptide could help manage body weight, a
crucial component in treating metabolic syndrome and preventing associated complications such as type 2
diabetes and cardiovascular diseases.
Moreover, the potential neuroprotective effects of
(Met5,Pro6,D-Phe7,D-Trp9,Phe10)-α-MSH (5-13) imply its use in neuroprotection strategies against
conditions like Alzheimer's disease and Parkinson's disease. The anti-inflammatory properties and
ability to reduce oxidative stress in neural tissues provide a basis for further exploration into how it
might preserve neuronal health and function, slowing the progression of neurodegenerative
symptoms.
Another investigative field for this peptide is its role in wound healing. The
interaction with melanocortin receptors, particularly MC5R, has been linked to enhanced tissue repair
processes. In cases of chronic wounds or in patients with impaired healing capabilities, such as those
with diabetes mellitus, the peptide could support acceleration of wound closure and tissue
regeneration.
While these potential applications are promising, the transition from experimental
research to clinical practice requires extensive trials and careful evaluation to ensure efficacy and
safety. The broad range of physiological roles influenced by the melanocortin system reflects the
peptide's diverse therapeutic possibilities, but each application needs targeted research to optimize
dosing, delivery mechanisms, and long-term safety profiles. Given these promising avenues,
interdisciplinary research is crucial to fully harness its therapeutic potential across different
medical fields.
How is (Met5,Pro6,D-Phe7,D-Trp9,Phe10)-α-MSH (5-13) administered in research
settings, and what are the challenges associated with its delivery?
In research settings, the
administration of (Met5,Pro6,D-Phe7,D-Trp9,Phe10)-α-MSH (5-13) typically involves various methods
tailored to the goals of the study and the specific physiological systems targeted. One common approach
is subcutaneous injection, which facilitates direct absorption into the bloodstream, allowing for
systematic interaction with melanocortin receptors throughout the body. This method is advantageous for
its fairly rapid onset of action and relative ease of controlled dosing.
Intravenous injection is
another method employed in research to achieve immediate systemic circulation and higher
bioavailability, especially in studies focusing on central nervous system effects or conditions where
swift impact is crucial. Intranasal delivery is also explored due to its potential to transport the
peptide directly to the brain by bypassing the blood-brain barrier. This route can be particularly
beneficial in neurological studies, emphasizing conditions such as cognitive disorders or
neurodegeneration.
Topical application may be researched for dermatological purposes, where
direct skin application can target melanocytes and potentially reduce systemic side effects. This method
is considered for pigmentation-related studies and healing of surface-level wounds.
Despite these
methods, several challenges in the peptide’s delivery are still under investigation. One primary issue
is its stability, as peptides are generally prone to enzymatic degradation once administered, which can
significantly affect efficacy and duration of activity. Therefore, enhancing peptide stability in vivo
through chemical modification or using carrier systems such as liposomes or nanoparticles is an active
area of research.
Furthermore, determining the appropriate dosing regimen is critical, as the
therapeutic window for peptides can be narrow, and inappropriate dosing might lead to adverse effects or
reduced therapeutic benefit. Establishing optimal dosing parameters involves complex pharmacokinetic and
pharmacodynamic assessments, often requiring sophisticated modeling and analysis.
Another
challenge is the potential immune response elicited by peptide administration, possibly resulting in
adverse reactions like hypersensitivity or neutralizing antibodies, which can limit the peptide's
effectiveness over time. To address this, researchers are investigating the design of peptide analogs
that retain therapeutic efficacy while minimizing immunogenicity.
Lastly, patient-specific
factors such as age, existing medical conditions, and concurrent medications must be considered, as
these could influence peptide absorption, distribution, metabolism, and excretion. Personalized delivery
solutions may eventually be necessary to accommodate these variability factors.
In summary, while
multiple administration routes are being explored, the delivery of (Met5,Pro6,D-Phe7,D-Trp9,Phe10)-α-MSH
(5-13) in research remains nuanced, requiring ongoing methodological advancements to mitigate challenges
such as stability, dosing accuracy, immune response, and individual variability.
What research is
needed to explore the long-term effects and safety of (Met5,Pro6,D-Phe7,D-Trp9,Phe10)-α-MSH (5-13) in
therapeutic applications?
The exploration of long-term effects and safety of
(Met5,Pro6,D-Phe7,D-Trp9,Phe10)-α-MSH (5-13) in therapeutic applications demands comprehensive research
attention across several domains. Primarily, longitudinal studies are essential to assess the enduring
impacts of the peptide over extended periods. Such studies need to focus on observing any potential
delayed adverse effects that may not be apparent in short-term analyses. The goal is to gather data that
can inform on chronic use scenarios, especially given the peptide’s broad interaction with melanocortin
receptors, implicating several physiological systems.
Detailed toxicity studies need to be
undertaken to determine safe dosage ranges. These studies should investigate both acute and chronic
dosing regimens to identify possible toxicological thresholds and understand the risk profile associated
with long-term administration. This information is crucial in formulating guidelines that clinicians can
follow to minimize the risk of adverse reactions in patients.
An understanding of the peptide’s
pharmacokinetics and pharmacodynamics over time is equally important. This includes investigating how
the body metabolizes and excretes the peptide with prolonged use. It’s vital to identify any potential
for accumulation in tissues or interaction with other bodily processes. Such pharmacological studies
will contribute significantly to determining safe and effective dosing practices, while highlighting any
interactions that may alter the peptide’s therapeutic profile.
Further research should also focus
on potential immunogenic responses to long-term treatment, including the development of anti-drug
antibodies that may neutralize the peptide’s effectiveness or cause immune-mediated side effects.
Techniques to modulate or reduce immunogenicity, potentially through structural modifications or
formulation adjustments, are an integral part of ensuring safety.
In addition to safety studies,
efficacy assessments are needed to confirm the peptide’s benefits over time. Continued monitoring of its
therapeutic effects in mitigating symptoms, improving clinical outcomes, and enhancing quality of life
for patients is crucial. Comparative studies with existing treatment options would help establish the
peptide’s position within therapeutic protocols, assessing whether it offers superior benefits or fewer
risks.
Regulatory considerations also play a role in the transition from research to clinical
applications. Following compliance with guidelines provided by authorities such as the FDA or EMA is
essential, ensuring that all safety assessments align with drug development protocols and
standards.
Lastly, patient-group specific studies might be required. Since individual responses
to peptide-based therapies can vary significantly, research tailored to different demographics,
including age, sex, underlying health conditions, and genetic background, should be conducted to
establish well-rounded safety and efficacy profiles across diverse populations.
Overall, the
pathway to understanding the long-term effects and safety of (Met5,Pro6,D-Phe7,D-Trp9,Phe10)-α-MSH
(5-13) necessitates multifaceted research endeavors, integrating toxicology, pharmacology,
immunogenicity, and efficacy analyses to ensure comprehensive evaluation for its potential therapeutic
applications.