Shaanxi BLOOM Tech Co., Ltd. is one of the most experienced manufacturers and suppliers of met-enkephalinamide cas 60117-17-1 in China. Welcome to wholesale bulk high quality met-enkephalinamide cas 60117-17-1 for sale here from our factory. Good service and reasonable price are available.
Met-enkephalinamide, a biologically active peptide derivative, belongs to the larger family of opioid peptides, renowned for their role in modulating pain perception, emotional responses, and regulating neurotransmitter release within the central and peripheral nervous systems. This specific compound, an amidated form of Met-enkephalin, undergoes minimal structural modification yet retains potent pharmacological properties.By replacing the terminal carboxylic acid group with an amide in Met-enkephalin, it exhibits enhanced stability against enzymatic degradation, allowing it to persist longer in biological milieus. This stability enhancement translates into potentially more sustained pharmacological effects, including analgesia (pain relief), sedation, and modulation of mood and appetite.
It acts primarily through binding to opioid receptors, particularly the mu (μ) and delta (δ) subtypes, initiating intracellular signaling cascades that lead to a variety of physiological responses. Its therapeutic potential has been explored in the treatment of chronic pain conditions, where it may offer an alternative to traditional opioid analgesics with fewer side effects, such as addiction liability and respiratory depression.
However, despite its promising properties, its clinical development has been limited due to challenges in delivering these peptides effectively across the blood-brain barrier and achieving adequate bioavailability. Ongoing research focuses on optimizing delivery systems and exploring its potential in combination therapies to harness its full therapeutic potential.
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Met-enkephalinamide COA
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| Certificate of Analysis | ||
| Compound name | Met-Enkephalinamide | |
| Grade | Pharmaceutical grade | |
| CAS No. | 60117-17-1 | |
| Quantity | 38g | |
| Packaging standard | PE bag+Al foil bag | |
| Manufacturer | Shaanxi BLOOM TECH Co., Ltd | |
| Lot No. | 202601090056 | |
| MFG | Jan 9th 2026 | |
| EXP | Jan 8th 2029 | |
| Structure |
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| Item | Enterprise standard | Analysis result |
| Appearance | White or almost white powder | Conformed |
| Water content | ≤5.0% | 0.26% |
| Loss on drying | ≤1.0% | 0.19% |
| Heavy Metals | Pb≤0.5ppm | N.D. |
| As≤0.5ppm | N.D. | |
| Hg≤0.5ppm | N.D. | |
| Cd≤0.5ppm | N.D. | |
| Purity (HPLC) | ≥99.0% | 99.89% |
| Single impurity | <0.8% | 0.42% |
| Total microbial count | ≤750cfu/g | 450 |
| E. Coli | ≤2MPN/g | N.D. |
| Salmonella | N.D. | N.D. |
| Ethanol (by GC) | ≤5000ppm | 550ppm |
| Storage | Store in a sealed, dark, and dry place below -20°C | |
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| Chemical Formula | C27H36N6O6S |
| Exact Mass | 572.24 |
| Molecular Weight | 572.68 |
| m/z | 572.24 (100.0%), 573.25 (29.2%), 574.24 (4.5%), 574.25 (4.1%), 573.24 (2.2%), 575.24 (1.3%), 574.25 (1.2%) |
| Elemental Analysis | C, 56.63; H, 6.34; N, 14.68; O, 16.76; S, 5.60 |
Biological Activity and Receptor Interaction&Research Applications
Opioid Receptor Agonist: Acting as a δ (delta) and ζ (zeta) opioid receptor agonist. This means met-enkephalinamide binds to and activates these receptors, leading to various biological effects.
Inhibitory Effects: It has been shown to inhibit pelvic nerve-evoked contractions of the distal colon in cats, with an IC50 value of 2.2 nM, indicating potent inhibitory activity at low concentrations.
Neuroscience: Due to its opioid receptor agonism, it is used in neuroscience research to study the mechanisms of pain modulation, addiction, and other opioid-mediated processes.
Cell Culture: At concentrations such as 0.1 nM, 10 nM, and 1 μM, it significantly reduces the total number of glial cells in culture, making it a valuable tool for studying glial cell biology.
Pharmacological Studies: It serves as a lead compound for the development of novel analgesics and drugs targeting opioid receptors.
Drug Development&Materials Science and Nanotechnology&Other Research Areas
Drug Candidates: It and its derivatives are explored as potential drug candidates for the treatment of pain, addiction, and other conditions where opioid receptor modulation is desired.
Preclinical Studies: It undergoes preclinical testing to evaluate its efficacy, safety, and pharmacokinetics, paving the way for potential clinical trials.
Polypeptide Modification: Used in the synthesis and modification of polypeptides, which find applications in materials science, such as the development of novel biomaterials.
Nanotechnology: Its unique chemical properties make met-enkephalinamide a suitable candidate for use in nanotechnology applications, including the design of drug delivery systems and targeted therapies.
Medical Research: Beyond neuroscience and pharmacology, it is also used in medical research to study various biological processes and diseases where opioid receptor modulation is implicated.
Biotechnology: It plays a role in biotechnology research, particularly in the development of novel biological tools and assays.
Pharmacological Effects
Opioid Receptor Agonist Activity
Delta (δ) Opioid Receptor Agonist: Acting as an agonist for the δ-opioid receptor, which is involved in various physiological processes. This interaction can lead to a range of effects, including modulation of pain perception, mood, and stress responses.
Zeta (ζ) Opioid Receptor Agonist (Putative): In addition to the δ-opioid receptor, it is also reported to be an agonist for the putative ζ-opioid receptor, although the exact role and function of this receptor are still under investigation.
Analgesic Effects
It exhibits analgesic (pain-relieving) properties by binding to opioid receptors, particularly the δ-receptor. This interaction can reduce pain perception and contribute to the overall analgesic effect.
It has been shown to inhibit pelvic nerve-evoked contractions in animal models, indicating its potential use in managing visceral pain.
Modulation of Neurotransmitter Release
By acting on opioid receptors, it can modulate the release of neurotransmitters such as norepinephrine, dopamine, and acetylcholine from neuronal terminals. This can have implications for various neurological and psychiatric conditions.
Immunomodulatory Effects
It has been shown to regulate immune function by interacting with opioid receptors on immune cells. This can lead to modulation of inflammatory responses and may have therapeutic potential in autoimmune and inflammatory diseases.
Effects on Cell Growth and Regeneration
As an endogenous ligand for opioid growth factor receptor (OGFR), it can regulate tissue growth and regeneration. This suggests its potential role in wound healing and tissue repair processes.
Neuroprotective Effects
By modulating neurotransmitter release and receptor activity, it may also exhibit neuroprotective effects, protecting neurons from damage caused by various insults such as oxidative stress and excitotoxicity.
Met-enkephalinamide is a bioactive peptide with important physiological and pharmacological effects. When conducting molecular structure analysis, we will delve into information on its composition of amino acids, secondary structure, spatial conformation, and receptor binding.
Composition of Amino Acids
The molecular structure is composed of five amino acids, including methionine (Met), phenylalanine (Phe), glycine (Gly), aspartic acid (Tyr), and alanine (Ala). These amino acids are arranged in a specific order within the peptide chain, determining their biological activity and specific structural functional relationships.
Secondary Structure
The secondary structure is one of its important structural features. Based on experimental data and theoretical models, we know that it tends to form β- Corner structure. This structure is stabilized by interactions such as hydrogen bonds and van der Waals forces, providing a basis for its effectiveness in living organisms.
Spatial Conformation
The spatial conformation is crucial for its binding to receptors and biological activity. Scientists have explored its possible spatial conformation through biophysical techniques such as nuclear magnetic resonance (NMR) and X-ray crystallography. These studies reveal its folding state and possible three-dimensional structure in solution, which helps us understand its mechanism of interaction with receptors.
Binding to Receptors
By binding to opioid receptors, it exerts its physiological effects such as pain relief and sedation. The receptor binding site interacts with a specific part of its molecular structure to form a stable coordination structure. This combination not only involves physical properties, but also involves interactions at multiple levels such as biochemistry and cellular signal transduction.
In summary, it's molecular structure is characterized by its pentapeptide nature, with a unique amino acid sequence including methionine, and the presence of specific functional groups such as peptide bonds, amino and amide groups, and a sulfur-containing side chain. These features contribute to its distinct chemical and biological properties.
1. Research Background of Endogenous Enkephalins
In the early 1970s, groundbreaking pharmacological studies verified the existence of specific opioid receptors in the mammalian central nervous system. Based on this finding, researchers hypothesized that corresponding endogenous analgesic ligands existed in organisms.
In 1975, British scientists Hughes and Kosterlitz extracted and isolated bioactive substances from porcine brain tissue. Combined with bioassay and amino acid sequencing, they successfully identified two functional pentapeptides: Met-enkephalin and Leu-enkephalin.
Their research was published in Nature, officially pioneering the research field of endogenous opioid peptides and laying a foundation for investigations on neural analgesic mechanisms.
2. Development and Creation of the Amidated Derivative
Native Met-enkephalin bears a critical flaw: its free C-terminal carboxyl group is rapidly hydrolyzed by endogenous peptidases, resulting in an in vivo half-life of merely several seconds and extremely poor biological stability, which renders it unsuitable for long-term pharmacological experiments and mechanistic studies.
To address this limitation, multiple international peptide research teams carried out structural optimization between 1976 and 1977 by modifying the free C-terminal carboxylic acid into an amide moiety, artificially generating met-enkephalinamide.
This derivative retains the excellent receptor affinity of the parent peptide while exhibiting drastically enhanced anti-hydrolysis capacity and stable biological activity. It has become a core tool peptide for opioid receptor research and analgesic mechanism exploration, and also provides critical theoretical support for the development of long-acting analgesic peptide drugs.
1. Dominant Synthetic Process
The peptide sequence of the product is Tyr-Gly-Gly-Phe-Met-NH₂. At present, Fmoc solid-phase peptide synthesis (SPPS) serves as the core preparation technology. Rink amide resin is selected as the solid support, which can directly construct the C-terminal amide structure and eliminate the cumbersome post-synthetic ammonolysis step required in conventional processes.
Synthesis initiates from the C-terminal methionine. Fmoc-protected methionine is first loaded onto the resin, followed by catalytic coupling and methanol capping to block unoccupied active sites. After removing amino protecting groups with piperidine solution, phenylalanine, two glycine residues and tyrosine are sequentially coupled in cycles. The phenolic hydroxyl group of tyrosine is masked with tert-butyl to suppress side reactions.
The HATU/DIPEA activation system is adopted throughout the whole procedure, combined with double-coupling protocol to guarantee high condensation efficiency.
Upon completion of peptide chain assembly, a mixed trifluoroacetic acid cleavage cocktail is used to cleave the peptide-resin linkage and remove side-chain protecting groups. Crude peptide is obtained via precipitation in cold diethyl ether and centrifugation. High-purity finished product is finally harvested after reverse-phase HPLC purification and lyophilization.
2. Comparative Process Advantages
Fmoc solid-phase synthesis presents prominent merits compared with the early Boc liquid-phase synthesis. Conventional liquid-phase synthesis involves complicated protecting group interconversion and an extra ammonolysis step for amidation, featuring laborious operation, heavy material loss and an overall yield below 15%.
By contrast, the optimized solid-phase synthesis delivers simple operation, minimal by-products and easily controllable reaction conditions, with a total yield ranging from 35% to 45% and consistent product purity exceeding 98%. It fully meets the demands of mass production with high purity for pharmacological research and laboratory preparation, and has become the standardized synthetic process universally adopted in the industry.
FAQ
Why is it called a 'research toxin'? --The 'cliff effect' of lethal dose administered intravenously
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It is an extremely potent peptide opioid receptor agonist, with a median lethal dose (LD ₅₀) as low as 20-30 mg/kg for intravenous administration. For untrained organisms, the window between lethal dose and effective analgesic dose is extremely narrow. Unlike natural Met enkephalin, which is completely destroyed in plasma within minutes, its amidation modification endows it with astonishing enzyme stability. This stability allows drugs to accumulate continuously in the body, which can easily lead to fatal respiratory depression. This is the fundamental reason why it is difficult to see in ordinary research laboratories - the risk return ratio determines that it is not suitable for use as a conventional tool. Behind the "scientific research use only" on the product information page is a true warning of this "toxin grade" pharmacological effect.
Is its' amide tail 'really just used to prevent degradation? --The switch from "agonist" to "antagonist"
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C-terminal amidation is not only a "shield" against degradation, but also a molecular switch that regulates pharmacological functions. Minor modifications on tyrosine residues can switch to complete antagonist activity on the same backbone. A groundbreaking study in 1987 revealed that when the tyrosine residue of Met enkephalin amide is replaced by meta tyrosine (m-Tyr) or N-phenethyl meta tyrosine, the molecule loses its excitatory activity while maintaining high affinity for the μ - opioid receptor (similar binding ability to morphine), flipping into a potent and selective antagonist. This indicates that the amide group provides a rigid 'docking platform' for the receptor, allowing subtle changes in the side chain to determine whether the signaling pathway is' on 'or' off '.
Does it hit itself in the solution? --The "self quenching" trap of nanoscale aggregation
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In high concentration stock solutions (such as those prepared with DMSO), molecules will self aggregate through π - π stacking of aromatic amino acids (tyrosine, phenylalanine), a phenomenon known as "self quenching". The measurement results indicate that although its solubility in PBS (pH 7.2) is 2 mg/mL, its solubility in DMSO is higher (10 mg/mL). However, this' high concentration 'is a double-edged sword. Once transferred to an aqueous buffer, it rapidly forms nanoscale aggregates due to hydrophobic interactions. This aggregation not only physically blocks the enzyme cleavage site (resulting in low enzyme kinetics experimental readings), but may also lead to abnormally high background fluorescence signals (due to energy transfer between tyrosine residues), seriously affecting the accuracy of experimental results.
Why is it not recommended to dissolve it in "pure water" storage? --The 'orphan peptide' that self devours
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In pure water lacking buffer salts and carrier proteins, its half-life may only be a few hours, as the lack of counter ions can lead to "self catalytic" degradation of amino and carboxyl groups within its molecules. As a charged small peptide, its stability in aqueous solution is highly dependent on ion strength and pH value. In pure water (especially deionized water), the lack of effective ion shielding leads to intense and irregular thermal motion of molecules, resulting in intramolecular or intermolecular nucleophilic attacks between the terminal primary amine and carboxyl group (forming diketopiperazine or similar compounds). The supplier's recommended storage conditions are 2-8 ° C dry and dark, which indirectly confirms their "pickiness" towards the solution environment. Once in an aqueous environment, it must be quickly used or strictly frozen.
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