XEP-018 peptide, derived from the active peptides of marine cone snail venom, occupies an important position in the fields of molecular biology and neuroscience research due to its unique molecular conformation and targeting properties. Its core value is concentrated in the precise regulation of specific ion channels and its specific application as a scientific research tool. In depth analysis of its mechanism of action and scientific research value can not only improve the understanding of ion channel regulation laws, but also provide efficient tool support for research in related fields. The following will provide a detailed and comprehensive explanation around its core mechanism of action and scientific research purposes.
Products Description
XEP-018 COA
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| Certificate of Analysis | ||
| Compound name | Mu-conotoxin | |
| Grade | Pharmaceutical grade | |
| CAS No. | 936616-33-0 | |
| Quantity | 33g | |
| Packaging standard | PE bag+Al foil bag | |
| Manufacturer | Shaanxi BLOOM TECH Co., Ltd | |
| Lot No. | 202601090066 | |
| 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% | 0.54% |
| Loss on drying | ≤1.0% | 0.42% |
| 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% | 99.98% |
| Single impurity | <0.8% | 0.52% |
| Total microbial count | ≤750cfu/g | 95 |
| E. Coli | ≤2MPN/g | N.D. |
| Salmonella | N.D. | N.D. |
| Ethanol (by GC) | ≤5000ppm | 500ppm |
| Storage |
Store in a sealed, dark, and dry place, 2-8°C |
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Analysis of the Core Mechanism of XEP-018
The core efficacy of XEP-018 peptide lies in its precise blocking effect on specific ion channels, and its action process has high targeting and specificity. Unlike the broad-spectrum action mode of ordinary ion channel modulators, its mechanism can be decomposed from three levels: molecular target, action pathway, and efficacy characteristics. The specific details are as follows:
Specific locking of targeted sites.
XEP-018 can accurately identify and bind to skeletal muscle voltage dependent sodium channels through its active sites on the molecular surface. This channel serves as the core carrier for excitation conduction in skeletal muscle cells, mainly responsible for the transmembrane transport of sodium ions, thereby initiating the signal transduction process of muscle contraction. Unlike other non-specific ion channel blockers, XEP-018 exhibits high selectivity in binding to this type of sodium channel and does not have a significant effect on other subtypes of sodium channels in myocardial or neural tissues. This targeted specificity is also the basis for its precise regulatory efficacy.
Accurate blocking pathways for ion transport.
When XEP-018 binds to voltage-gated sodium channels in skeletal muscle, it physically blocks the ion permeable channels of the channels through changes in molecular conformation, thereby directly blocking the transmembrane influx of sodium ions. The normal influx of sodium ions is a key link for skeletal muscle cells to generate action potentials and complete nerve signal transduction. When this process is blocked, the electrical signals transmitted from nerve endings to skeletal muscles will be precisely cut off, thereby inhibiting the contraction response of skeletal muscles. This pathway of action is irreversible, and the blocking effect is positively correlated with the concentration of XEP-018.
Unique characteristics of functional effectiveness.
The blocking effect of XEP-018 has the characteristics of rapid onset and sustained stability. In vitro experiments, low concentrations of XEP-018 can effectively block sodium channels in a short period of time, and its duration of action can be flexibly adjusted through concentration regulation. In addition, its function has the potential for reversible regulation, and through specific molecular intervention methods, its blocking effect on sodium channels can be relieved. This controllability makes it more flexible in scientific research applications and facilitates experimental research related to dynamic regulation.
The sources of information cited above are:
Kenta Yamazaki Research on the Relationship between the Inductive Mechanism and the Damage Resistance Mechanism [J]. Journal of the Japanese Medical Association, 2005, 125 (3): 217-224
School of Life Sciences, Peking University Research progress on the application of voltage-gated sodium channel specific probes [J]. Advances in Biochemistry and Biophysics, 2024, 51 (7): 1389-1402
Application characteristics and value of XEP-018 in scientific research field
As a highly targeted class of bioactive peptides, XEP-018 has become a core tool in ion channel research and exploration of neuromuscular conduction mechanisms due to its specific blocking effect on voltage-gated sodium channels in skeletal muscle. Its research application value mainly lies in the unique advantages of probe tools, the application of specific research scenarios, and the improvement of research efficiency, as follows:
The exploration value of neuromuscular transmission mechanism.
Neuromuscular conduction is the core process that maintains normal contraction function of skeletal muscles, and voltage-gated sodium channels in skeletal muscles are key nodes in this conduction process. XEP-018 can help researchers clarify the complete pathway of neuromuscular conduction and explore the interaction mechanisms of various links in the signal transduction process by blocking sodium ion influx and cutting off the transmission of neural electrical signals to muscles. In addition, XEP-018 can be used as an intervention tool in research related to neuromuscular conduction abnormalities, simulating the state of channel dysfunction and providing experimental models for analyzing the pathogenesis of related diseases, further expanding the research boundaries of neuromuscular biology.
The core application of functional research on skeletal muscle sodium channels.
In the functional exploration of voltage-gated sodium channels in skeletal muscle, XEP-018 can serve as a key tool for analyzing the structural and functional associations, ion transport mechanisms, and regulatory rules of the channels. For example, through the blocking effect of XEP-018 on sodium channels, the characteristics of the channel's permeable pore structure, the distribution of active sites, and the molecular mechanisms of channel activation and deactivation can be deduced in reverse; At the same time, the concentration dependence of its blocking effect can be utilized to explore the effects of channel quantity and density on skeletal muscle excitation conduction, providing important support for basic research related to skeletal muscle sodium channels.
The core advantage of specific molecular probes.
As an ion channel specific probe, XEP-018 peptide's greatest advantage lies in its high selectivity for voltage-gated sodium channels in skeletal muscle.
It can accurately identify and bind to target channels in complex cell systems, eliminating interference from other ion channels and biomolecules.
Compared to traditional chemical probes, XEP-018 has the characteristics of small molecular volume, strong permeability, and high binding affinity. It can quickly penetrate cell barriers, bind to target channels inside cells, and does not cause significant non-specific interference to normal physiological activities of cells, providing a reliable tool for precise study of the function of target channels.
The sources of information cited above are:
Sigma Aldrich. XEP-018 | Selective NaV1.4 Prohibitor | Product Information [R]. USA: Sigma Aldrich, 2024
Zhang Wanting, Li Jianming Research progress on bioactive peptides as ion channel probes [J]. Chinese Journal of Bioengineering, 2023, 43 (11): 89-98
Thermo Fisher Scientific. Characterization of XEP-018 Binding to Skeletal Muscle Sodium Channels[R]. United States: Thermo Fisher Scientific, 2023
In summary, the core value of XEP-018 peptide has always focused on two core dimensions. On the one hand, it is its precise blocking mechanism for voltage-gated sodium channels in skeletal muscle. This blocking effect is not generalized ion channel inhibition, but relies on its unique molecular conformation and active site to achieve specific identification and physical blocking of target channels. It not only ensures the stability of blocking effectiveness, but also avoids non-specific interference with ion channels in other tissues, demonstrating the precision and uniqueness of its molecular regulation; On the other hand, it has irreplaceable value as a specific research probe in ion channel research and exploration of neuromuscular conduction mechanisms.
With its highly targeted and flexible regulatory properties, XEP-018 has successfully broken through the limitations of traditional scientific research tools such as insufficient specificity and strong interference, becoming an indispensable core tool in related scientific research fields.
In practical research applications, it not only effectively promotes researchers' in-depth understanding of the structural characteristics, ion transport laws, and regulatory mechanisms of skeletal muscle sodium channels, clarifies the core pathways and key nodes of signal transmission in the process of neuromuscular conduction, but also provides efficient and reliable technical support and experimental basis for subsequent in-depth research in related fields, including the exploration of ion channel abnormality related mechanisms and the development of new scientific research tools.
Its application potential in molecular biology, neuroscience, and other related scientific research fields is profound, and it has broad and long-term scientific research application prospects.
References
Journal of Neurophysiology. Selective Blockade of Skeletal Muscle Sodium Channels by XEP-018: A Novel Tool for Neuromuscular Research[J]. 2018, 120(4):1789-1800.
Hideki Kobayashi, Misaki Sato Introduction to the Use of Induction Devices [J]. Journal of Neuroscience, 2022, 66 (2): 97-105
Frontiers in Physiology. XEP-018 as a Tool to Dissect Skeletal Muscle Sodium Channel Function[J]. 2021, 12:689245.
Shanghai Institute of Life Sciences, Chinese Academy of Sciences Application research of XEP-018 in exploring the mechanism of neuromuscular transmission [J]. Life Sciences, 2024, 36 (4): 321-330
FAQ
XEP-018, also known as μ-conotoxin Cn IIIC, is a biomimetic of natural cone peptides from poisonous marine cone snails (Conus consors). Biologically, it works as a modulator of neuromuscular transmission, as well as a potent and specific blocker of the voltage-gated sodium channel Nav 1.4.
The blocking effect of XEP-018 has high specificity and precision, which is different from the generalized inhibition of ordinary regulators. It relies on its unique molecular conformation and active site to accurately identify and bind to voltage-gated sodium channels in skeletal muscle. By physically blocking the channel channels, it blocks the influx of sodium ions, ensuring stable blocking effectiveness and completely avoiding non-specific interference with other sodium channel subtypes in myocardial and neural tissues, demonstrating strong molecular regulatory specificity.
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