Taiy Chemical
Met-Enkephalin-RGL
Synonym Met-Enkephalin-RGL
Species Human
Protein Accession P01210
Purity Greater than 95%
Endotoxin Level Less than 1 EU/µg
Biological Activity The ED50 of ≤0.5ng/ml
Expression System E. coli
Fusion Tag None
Predicted Molecular Mass 5557 Da
Formulation Lyophilized from a 0.2 μm filtered solution of 20mM PB,150mM NaCl, pH7.2.
Reconstitution It is recommended to reconstitute the lyophilized Met-Enkephalin-RGL in sterile 18MΩ-cm H2O not less than 100µg/ml, which can then be further diluted to other aqueous solutions.
Storage & Stability Store lyophilized protein at -20°C. Aliquot the product after reconstitution to avoid repeated freezing/thawing cycles. Reconstituted protein can be stored at 4°C for a limited period of time. The lyophilized protein remains stable until the expiry date when stored at -20°C.
FAQ
What is Met-Enkephalin-RGL and how does it work in the body?
Met-Enkephalin-RGL is a synthetic analog of the naturally occurring peptide Met-enkephalin, which is one of the endogenous opioids found in the body. Enkephalins are part of a broader group of peptides known as endorphins, which play key roles in modulating pain and producing analgesia. Met-Enkephalin specifically binds to the delta and mu-opioid receptors in the central nervous system. This binding alters the perception of pain by inhibiting the release of neurotransmitters involved in the transmission of pain signals, effectively reducing the sensation of pain. Its potency and specificity for opioid receptors make it an important peptide for research into pain management and potential therapeutic applications. The addition of RGL, a modified amino acid sequence, is designed to enhance the peptide’s stability and resistance to enzymatic degradation. This modification allows it to remain active longer in the body, potentially increasing its therapeutic benefits and making it more suitable for clinical applications. The improved stability and activity duration mean that Met-Enkephalin-RGL can be administered less frequently while providing sustained effects.

In addition to pain modulation, Met-Enkephalin-RGL is also being explored for its potential effects on the immune system. Research suggests that opioids have immunomodulatory properties, and Met-Enkephalin-RGL might influence the activity of immune cells, thereby affecting inflammation and immune response. This dual action on pain and the immune system presents a significant opportunity for treating conditions that involve chronic pain and inflammation. Furthermore, the peptide’s potential applications extend beyond just analgesia, including areas such as mood disorders, stress response, and potentially neurodegenerative diseases, because of its interaction with neurotransmitter systems in the brain. Although still under investigation, Met-Enkephalin-RGL signifies a promising pathway in developing advanced therapeutic agents that harness the multifaceted roles of enkephalins within the physiological and neurological framework.

What are the potential benefits of using Met-Enkephalin-RGL over traditional pain management methods?
Met-Enkephalin-RGL offers a variety of potential benefits compared to traditional pain management techniques, primarily due to its mechanism of action and the nature of its composition. One of the most notable advantages is its specificity and targeted action on opioid receptors, allowing for more precise modulation of pain pathways. Traditional pain management often relies on non-steroidal anti-inflammatory drugs (NSAIDs) or non-specific opioids. While effective, these medications can bring about significant side effects such as gastrointestinal issues, potential for addiction, or liver toxicity with long-term use. Met-Enkephalin-RGL, due to its selective activity, may reduce these side effects and offer a safer profile for long-term management of chronic pain.

Furthermore, Met-Enkephalin-RGL’s modified structure—enhanced by the RGL sequence—gives it improved stability over time, meaning it can remain active in the body far longer than naturally occurring enkephalins. By resisting enzymatic breakdown, this synthetic analog sustains its analgesic effects with less frequent dosing. This increased duration not only is more convenient for patients but may also lead to better adherence to treatment protocols with improved overall outcomes. Moreover, unlike common narcotic painkillers, Met-Enkephalin-RGL is being developed and studied with the aim of minimizing or even avoiding the development of tolerance and physical dependence. This could be of particular importance when addressing the challenges associated with opioid addiction and abuse, a significant concern with current opioid use.

In addition to its role in pain relief, the immunomodulatory effects of Met-Enkephalin-RGL suggest it may concurrently manage both pain and inflammation, which is not typically achievable with conventional analgesic treatments. This dual functionality can be particularly valuable in managing conditions such as rheumatoid arthritis, where both pain and inflammation are constant issues. The combined pain relief and modulation of the immune response also hold promise for synergistic effects that enhance patient quality of life. Ongoing research continues to explore these multifaceted benefits, potentially propelling Met-Enkephalin-RGL toward more widespread clinical application. Ultimately, while requiring further trials and studies to fully understand and validate its benefits, the peptide's promising profile offers a glimpse into next-generation pain management solutions.

How does the modification in Met-Enkephalin-RGL result in enhanced stability compared to natural Met-Enkephalin?
The modification in Met-Enkephalin-RGL is designed specifically to enhance the peptide's stability, making it a powerful candidate in therapeutic development. Naturally occurring Met-enkephalin, like many other peptides, is susceptible to rapid enzymatic degradation in the bloodstream, which can significantly limit its clinical efficacy. This degradation is primarily carried out by peptidases that break down peptide bonds, thus inactivating the therapeutic agent. The addition of the RGL sequence in Met-Enkephalin-RGL is a strategic modification aiming to overcome such limitations and prolong the bioactive lifespan of the peptide.

The RGL sequence is thought to confer resistance against these enzyme activities, allowing Met-Enkephalin-RGL to evade premature breakdown. This is achieved through structural alterations that cause steric hindrance or alter the secondary structure of the peptide, making it a less suitable substrate for peptidases. Consequently, this modification helps maintain the integrity of Met-Enkephalin-RGL in the circulatory system, providing a longer duration of action which is highly beneficial in clinical settings where reduced frequency of dosing is advantageous.

Another aspect of the enhanced stability is related to improved binding affinity and specificity for opioid receptors. The modification may simultaneously facilitate better interaction with the target receptors, implying more pronounced and sustained pharmacological effects. The ability to remain bonded to these receptors longer means enhanced signal transduction, which translates to more effective alleviation of pain and modulation of neurological responses. Moreover, this improved receptor interaction contributes to reduced off-target effects, minimizing potential adverse reactions commonly associated with traditional opioids and offering a cleaner safety profile.

Additionally, the prolonged bioavailability derived from enhanced stability does not only improve patient convenience but also potentiates engagement with downstream signaling pathways linked to opioid receptor activation. This could result in robust therapeutic outcomes such as sustained analgesia without reaching toxic levels that could initiate tolerance or dependence. The structural integration provided by modifications like that of the RGL sequence represents a frontier in peptide drug design, unlocking new possibilities for enhancing the functionality and therapeutic potential of peptide-based drugs like Met-Enkephalin-RGL beyond what is feasible with their natural counterparts.

Can Met-Enkephalin-RGL be used for conditions other than pain management, and if so, how?
Met-Enkephalin-RGL is primarily studied for its analgesic properties, but its biological activities suggest it could be applicable in a range of other therapeutic contexts beyond traditional pain management. One area under investigation is its potential role in managing mood disorders and stress-related conditions, such as depression and anxiety. Endogenous opioid peptides, including enkephalins, play an intrinsic role in regulating mood and emotional states by interacting with the neurotransmitter systems in the brain. By modulating these systems, Met-Enkephalin-RGL may help balance mood levels and alleviate symptoms associated with mood disorders, offering a novel approach compared to standard treatments like SSRIs.

Additionally, the immunomodulatory properties of Met-Enkephalin-RGL open the door to its use in managing inflammatory and autoimmune conditions. By influencing immune cell activity and cytokine production, this peptide could help regulate inflammatory responses and ameliorate symptoms of autoimmune diseases such as rheumatoid arthritis and multiple sclerosis. This capacity to modulate the immune system highlights its dual-action potential, making it a candidate for combined anti-inflammatory and analgesic therapy, a layered approach often required in complex chronic conditions.

Another promising application lies in the area of neuroprotection and neurodegenerative diseases. Through its interaction with opioid receptors, Met-Enkephalin-RGL could exert neuroprotective effects that help slow the progression of neurodegenerative disorders like Parkinson's or Alzheimer's disease. This potential is based on the peptide’s ability to mitigate cellular stress responses and modulate pathways related to cellular survival and apoptosis. While clinical validation is still pending, the incorporation of such peptides in comprehensive treatment regimens could signal a shift in tackling the multifactorial nature of neurodegenerative diseases.

Moreover, there is interest in exploring Met-Enkephalin-RGL's role in addiction therapy. Its design aims to reduce the development of tolerance and dependency, making it a potentially safer alternative for those seeking relief from substance addiction. By possibly modulating reward pathways without the same addictive potential as conventional opioids, Met-Enkephalin-RGL could contribute to strategies aimed at reducing opioid dependence. The development of treatments capable of addressing withdrawal symptoms and reducing cravings without perpetuating addiction could be a significant breakthrough.

Met-Enkephalin-RGL's versatility exemplifies the potential of peptide-based treatments to address a spectrum of conditions, thanks to their specificity, efficacy, and lower side-effect profiles. Continued research is crucial to fully elucidate its capabilities and pave the way for innovative therapeutic strategies that leverage its unique properties. While further clinical trials are needed for these alternative applications, the prospects they represent could redefine our approach to managing complex and multi-faceted health challenges.

What makes Met-Enkephalin-RGL a promising candidate for future pharmaceuticals?
Met-Enkephalin-RGL stands out as a promising candidate in the pharmaceutical landscape due to several intrinsic factors attributed to its unique composition and mode of action. The peptide leverage on its specificity and potency makes it a powerful tool in the emerging field of peptide-based therapeutics. Unlike small molecule drugs, peptides like Met-Enkephalin-RGL offer a high degree of specificity in targeting biological processes. They can engage with receptors or enzymes with precision, leading to fewer off-target effects and consequently a lower incidence of adverse reactions. This characteristic is incredibly appealing in drug development as it aligns with the ongoing demand for safer and more targeted therapies.

Moreover, Met-Enkephalin-RGL’s enhanced stability and prolonged duration of action represent a significant advancement in peptide therapeutics. Traditional peptides often suffer from rapid degradation in vivo, limiting their therapeutic potential. However, by incorporating modifications that confer resistance to enzymatic breakdown, Met-Enkephalin-RGL overcomes these conventional barriers, offering a sustainable and effective means of achieving therapeutic effects. The ability to maintain its bioactivity over extended periods elevates its clinical utility by enabling less frequent dosing schedules, enhancing patient compliance, and delivering sustained results that improve overall treatment outcomes.

Another compelling feature of Met-Enkephalin-RGL is its inherent dual-action ability. As a peptide with effects on both pain and immune response, it encompasses a broad therapeutic window. The capacity to address multiple pathways or conditions with a single compound is highly sought after in medicine, particularly for comorbid conditions that commonly require complex treatment regimens. This attribute positions Met-Enkephalin-RGL as a versatile therapeutic candidate with the potential to simplify approaches to complex health issues and improve patient quality of life.

Beyond its current scope, Met-Enkephalin-RGL also reflects a major trend toward personalized medicine. Its design facilitates adjustment or refinement, allowing custom tailoring to fit specific patient needs or to enhance its interaction with biological targets. As precision medicine becomes more prevalent, the adaptability and specificity of peptides like Met-Enkephalin-RGL will play an instrumental role in creating customized and effective patient-centric therapies.

What's equally fascinating is the broad potential market that Met-Enkephalin-RGL presents. From pain management to autoimmune conditions, mood disorders, and potentially neurodegenerative diseases, Met-Enkephalin-RGL could serve a wide array of medical sectors. Such versatility means it could significantly influence the pharmaceutical industry by offering a strategic solution that is both effective and economical. Furthermore, given the ongoing opioid crisis and the urgent need for safer pain management solutions, Met-Enkephalin-RGL could fulfill a critical gap by providing alternative strategies that target pain without the high risk of addiction.

The evolution of Met-Enkephalin-RGL outlines a remarkable trajectory in the role of peptides within modern medicine. As further research and clinical trials unveil its full potential, it is poised to redefine therapeutic strategies, leading to safer, more effective, and personalized approaches to a wide range of health challenges.
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