Endotoxin inhibitor, also known as H-LYS-THR-LYS-CYS-LYS-PHE-LEU-LYS-LYS-CYS-OH, is a biological preparation used to inhibit or neutralize endotoxin activity. Usually presented as a white or almost white powdery substance, with a delicate texture that is easily soluble in water or physiological saline. Molecular formula C55H97N15O12S2, CAS 147396-10-9. Endotoxins are the main component of the cell wall of Gram negative bacteria.
When bacteria die or the cell wall ruptures, endotoxins are released into the surrounding environment, triggering a series of inflammatory reactions that may lead to serious health problems. Therefore, H-LYS-THR-LYS-CYS-LYS-PHE-LEU-LYS-LYS-CYS-OH have broad application prospects in the fields of medicine and bioscience. It usually has good biocompatibility and does not exhibit significant immune reactions or toxic effects on human tissues and cells. Meanwhile, its safety has been fully validated through rigorous clinical trials and safety assessments. This makes it have lower side effects and higher safety in clinical applications.
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Endotoxin Inhibitor COA
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| Certificate of Analysis | ||
| Compound name | Endotoxin Inhibitor | |
| Grade | Pharmaceutical grade | |
| CAS No. | 147396-10-9 | |
| Quantity | 22g | |
| Packaging standard | PE bag+Al foil bag | |
| Manufacturer | Shaanxi BLOOM TECH Co., Ltd | |
| Lot No. | 202601090088 | |
| 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% | 0.22% |
| Loss on drying | ≤1.0% | 0.27% |
| 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% | 99.80% |
| Single impurity | <0.8% | 0.47% |
| Total microbial count | ≤750cfu/g | 555 |
| E. Coli | ≤2MPN/g | N.D. |
| Salmonella | N.D. | N.D. |
| Ethanol (by GC) | ≤5000ppm | 662ppm |
| Storage | Store in a sealed, dark, and dry place below -15°C | |
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| Chemical Formula | C55H97N15O12S2 |
| Exact Mass | 1223.69 |
| Molecular Weight | 1224.59 |
| m/z | 1223.69 (100.0%), 1224.69 (59.5%), 1225.69 (17.4%), 1225.68 (9.0%), 1224.69 (5.5%), 1226.69 (5.4%), 1226.70 (3.3%), 1225.69 (3.3%), 1225.69 (2.5%), 1224.69 (1.6%), 1227.69 (1.6%), 1226.70 (1.5%), 1224.69 (1.1%) |
| Elemental Analysis | C, 53.94; H, 7.98; N, 17.16; O, 15.68; S, 5.24 |
Endotoxin inhibitor, is a class of compounds with special biological activity that can specifically bind and inhibit the activity of endotoxins. Endotoxins, as the main component of the cell wall of Gram negative bacteria, can be released into the environment during bacterial death or cell wall rupture, causing strong inflammatory reactions and various diseases. Therefore, H-LYS-THR-LYS-CYS-LYS-PHE-LEU-LYS-LYS-CYS-OH has broad application prospects in fields such as medicine, biotechnology, and public health.
1. Inhibiting inflammatory response
Endotoxins are strong inflammatory triggers that can activate the body's immune system, leading to the occurrence of inflammatory reactions. It inhibits the occurrence of inflammatory reactions by binding to endotoxins, blocking their interaction with cell surface receptors. This feature makes it have important application value in the treatment of inflammatory diseases caused by endotoxins, such as sepsis, septic shock, etc.
2. Protecting tissues and organs
Inflammatory reactions caused by endotoxins can lead to damage and dysfunction of tissues and organs. H-LYS-THR-LYS-CYS-LYS-PHE-LEU-LYS-LYS-CYS-OH reduces the degree of damage to tissues and organs by inhibiting inflammatory reactions, protecting their normal function. Research has shown that it has a protective effect on important organs such as the heart, lungs, liver, and kidneys, and can reduce the incidence of organ damage and dysfunction caused by endotoxins.
3. Regulating immune response
H-LYS-THR-LYS-CYS-LYS-PHE-LEU-LYS-LYS-CYS-OH can not only directly inhibit the activity of endotoxins, but also exert therapeutic effects by regulating the body's immune response. It can affect the activation and proliferation of immune cells, regulate the production and release of inflammatory mediators, thereby balancing the body's immune response and avoiding excessive or insufficient immune response causing damage to the body.
4. Antibacterial effect
In addition to inhibiting the activity of endotoxins, some it also have antibacterial effects. They can destroy the cell wall or membrane of bacteria, interfere with their growth and reproduction, and thus achieve antibacterial purposes. This makes it have certain advantages in the treatment of bacterial infectious diseases.
5. Relieve symptoms of endotoxemia
Endotoxemia refers to a systemic inflammatory response caused by the accumulation of endotoxins in the body. H-LYS-THR-LYS-CYS-LYS-PHE-LEU-LYS-LYS-CYS-OH reduces the symptoms of endotoxemia, such as fever, chills, and hypotension, by inhibiting the activity of endotoxins. At the same time, it can also improve the prognosis of patients and increase survival rates.
6. Improving immune dysfunction
In some disease states, such as tumor and AIDS, the immune function of patients may be suppressed, resulting in the reduction of the body's resistance to pathogens such as endotoxin. H-LYS-THR-LYS-CYS-LYS-PHE-LEU-LYS-LYS-CYS-OH regulates immune responses, improves immune dysfunction, enhances the body's resistance to pathogens, and helps prevent infections and diseases.
7. Drug development
Based on the aforementioned functions of H-LYS-THR-LYS-CYS-LYS-PHE-LEU-LYS-LYS-CYS-OH, it can serve as a drug candidate for the treatment of various diseases caused by endotoxins. Through further research and optimization, it is expected to develop H-LYS-THR-LYS-CYS-LYS-PHE-LEU-LYS-LYS-CYS-OH drugs with high efficiency, low toxicity, and strong specificity, providing more options for clinical treatment.
8. Application of Biotechnology
H-LYS-THR-LYS-CYS-LYS-PHE-LEU-LYS-LYS-CYS-OH also has broad application prospects in the field of biotechnology. For example, it can be used as an additive in biomaterials to improve their biocompatibility and safety; It can also serve as a recognition element for biosensors to detect and monitor the content and activity of endotoxins.
9. Public health prevention and control
Endotoxins are one of the important pathogens of many infectious diseases, so endotoxin inhibitor also have certain application value in public health prevention and control. It can be used to prevent and control infectious diseases caused by endotoxin, such as septicemia, septic shock, etc., and help reduce the incidence rate and mortality of diseases.
As a class of compounds that can specifically bind and inhibit endotoxin activity, have broad application prospects in the pharmaceutical field. As one of the important methods for preparing it, chemical synthesis has the advantages of controllable reaction and clear product structure.
Synthesis steps and chemical equations:
1. Preparation of starting materials
The selection of starting materials is crucial for the entire synthesis process. Using simple organic compounds such as alcohols, amines, carboxylic acids, etc. as starting materials, the skeleton of the target compound is gradually constructed through a series of chemical reactions. For example, appropriate alcohols and amines can be selected for condensation reactions to generate amide compounds as starting materials for subsequent reactions.
ROH+R'NH2 → RCONHR '+H2O
2. Protection and Unprotection Steps
During the synthesis process, certain functional groups may need to be protected to avoid unnecessary side reactions. Common protective groups include tert butoxycarbonyl (Boc), benzyloxycarbonyl (Cbz), etc. The protective step usually involves a reaction with the protective group, while the deprotection step involves the removal of the protective group.
RNH2+(Boc) 2O → RNHBoc+HOBoc
RNHBoc+HCl → RNH2+Boc Cl
3. Transformation and Modification of Functional Groups
By transforming and modifying functional groups, the structure and properties of the compound can be further adjusted to meet the activity requirements of H-LYS-THR-LYS-CYS-LYS-PHE-LEU-LYS-LYS-CYS-OH. Common functional group transformations include oxidation, reduction, halogenation, alkylation, etc.
RCHO+O2 → RCOOH
4. Formation and fracture of bonds
In the process of constructing the skeleton of H-LYS-THR-LYS-CYS-LYS-PHE-LEU-LYS-LYS-CYS-OH, specific chemical bonds need to be formed, such as carbon carbon bonds, carbon nitrogen bonds, etc. This usually involves reactions such as nucleophilic substitution, electrophilic substitution, and addition. At the same time, it may also be necessary to break certain chemical bonds to achieve structural reorganization.
RX+Nu- → RNu+X-
5. Generation and purification of terminal products
After the above steps, the final product of endotoxin inhibitor is generated. By using appropriate purification methods such as crystallization, recrystallization, column chromatography, etc., the purity and yield of the product can be improved.
C55H97N15O12S2 (crude) → C55H97N15O12S2 (pure)
The endotoxin lipopolysaccharide molecule is composed of three parts: bacterial specific polysaccharides, non-specific core polysaccharides, and lipid A. Lipid A is the main toxic component of endotoxins. The lipid A structure of different Gram negative bacteria is basically similar. Therefore, for infections caused by Gram negative bacteria, although the species may vary, the toxic effects caused by endotoxins are generally similar. These toxic reactions mainly include:
The human body is extremely sensitive to bacterial endotoxins. A very small amount (1-5 nanograms per kilogram of body weight) of endotoxin can cause an increase in body temperature, and the fever reaction lasts for about 4 hours before gradually subsiding. During natural infection, due to the continuous growth and reproduction of Gram negative bacteria, accompanied by gradual death and release of endotoxins, the fever reaction will continue until the pathogenic bacteria in the body are completely eliminated.
The reason why endotoxins cause fever reactions is that endotoxins act on macrophages, neutrophils, and other cells in the body, causing them to produce cytokines such as interleukin-1, interleukin-6, and tumor necrosis factor alpha. These cytokines act on the thermoregulatory center of the host hypothalamus, promoting an increase in body temperature and fever.
After bacterial endotoxins enter the host's body, the number of neutrophils, which account for 60-70% of the total white blood cells in the bloodstream, rapidly decreases because the cells move and adhere to tissue capillaries. However, 1-2 hours later, the neutrophil release factor induced by endotoxins stimulates the release of neutrophils from the bone marrow into the bloodstream, significantly increasing their numbers. Some immature neutrophils are also released.
Salmonella typhi, a Gram negative bacterium, is an exception as its endotoxin consistently reduces the total white blood cell count. Due to the fact that the total number of white blood cells in the bloodstream increases in the vast majority of patients infected with Gram negative bacteria, doctors often need to test the patient's blood to determine the total number and classify white blood cells before diagnosis, in order to preliminarily distinguish between bacterial infection and viral infection. The total white blood cell count and neutrophil percentage of patients infected with the virus are generally within the normal range.
When a large number of Gram negative pathogens die in the lesion or bloodstream, releasing a large amount of endotoxins into the bloodstream, endotoxemia can occur. A large amount of endotoxins act on macrophages, neutrophils, endothelial cells, platelets, as well as complement and coagulation systems in the body, producing bioactive substances such as interleukin-1, interleukin-6, interleukin-8, tumor necrosis factor alpha, histamine, serotonin, prostaglandins, and kinins.
These substances act on small blood vessels, causing functional disorders and microcirculatory disorders. Clinical manifestations include microcirculatory failure, hypotension, hypoxia, acidosis, etc., leading to shock in patients. This pathological reaction is called endotoxin shock.
I. Foundation of Endotoxin Cognition (Late 19th Century – Mid-20th Century)
In 1892, Richard Pfeiffer first proposed the concept of "endotoxin", confirming it as a thermostable toxic component in the cell wall of Gram-negative bacteria that can induce sepsis and shock.
By the mid-20th century, studies identified lipid A as the core toxic structure of endotoxin. It was verified to trigger an inflammatory cytokine storm by activating the TLR4 receptor, laying a target foundation for the research and development of the product.
II. Early Exploration of Inhibitors (1970s–1990s)
Starting from the 1970s, scientists began to screen endotoxin antagonists.
In 1995, E5531, synthesized based on the non-toxic lipid A structure of Rhodopseudomonas bacteria, was developed.
It competitively binds to lipid A and blocks the interaction between endotoxin and its receptor, becoming the first high-efficiency synthetic endotoxin antagonist.
Meanwhile, antibiotics such as Polymyxin B were found to neutralize endotoxin via binding to lipid A, yet their clinical application is limited by nephrotoxicity.
III. Emergence of Specific Polypeptide Inhibitors (Early 21st Century)
At the beginning of the 21st century, the lipid A-targeted synthetic polypeptide the product was developed. It consists of 10 amino acids and contains a characteristic disulfide bond.
With high affinity binding to lipid A, it blocks the LPS-TLR4 signaling pathway and inhibits the release of pro-inflammatory factors including TNF-α and IL-6.
It also exhibits extremely low toxicity with an LD₅₀ greater than 1000 mg/kg. Since 2018, multiple animal experiments have proven that it can significantly reduce the mortality of mice in sepsis models, making it an important tool molecule for basic medical research and anti-inflammatory drug development.
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