Shaanxi BLOOM Tech Co., Ltd. is one of the most experienced manufacturers and suppliers of tiamulin powder in China. Welcome to wholesale bulk high quality tiamulin powder for sale here from our factory. Good service and reasonable price are available.
Tiamulin was first isolated from the fungus Clitopilus passeckerianus in the 1950s and later modified to enhance its stability and efficacy. The semisynthetic derivative, tiamulin hydrogen fumarate, was introduced in the 1970s as a veterinary antibiotic. Its approval for use in pigs and poultry marked a significant advancement in the management of respiratory and enteric diseases in these species.
Tiamulin, a semisynthetic derivative of the antibiotic pleuromutilin, has been a cornerstone in veterinary medicine for decades, particularly in the treatment of swine and poultry diseases. Its unique mechanism of action, broad-spectrum antimicrobial activity, and favorable pharmacokinetic properties make it a valuable tool in combating bacterial and mycoplasmal infections.
Additional information of chemical compound:
| Product Name | Tiamulin Powder | Tiamulin Injection | |
| Product Type | Powder | Injection | |
| Product Purity | >95% | >95% | |
| Product Specifications | 1g; 10g; 100g; 1kg | 10%/100ml;20%/100ml | |
| Product Form | Organic synthesis | injection | |
Tiamulin +. COA
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| Certificate of Analysis | ||
| Compound name | Tiamulin | |
| CAS No. | 55297-95-5 | |
| Quantity | 45kg | |
| Manufacturer | Shaanxi BLOOM TECH Co., Ltd | |
| Lot No. | 20250415012 | |
| MFG | Apr.15th2025 | |
| EXP | Apr.15th2028 | |
| Structure |
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| Item | Enterprise standard | Analysis result |
| Appearance | Off-white powder | Conformed |
| Water content | ≤5.0% | 0.13% |
| Heavy Metals | Pb≤0.5ppm | N.D. |
| As≤0.5ppm | N.D. | |
| Hg≤0.5ppm | N.D. | |
| Cd≤0.5ppm | N.D. | |
| Purity (HPLC) | >95%% | 99.95% |
| Single impurity | <0.8% | 0.16% |
| Total microbial count | ≤750cfu/g | 30 |
| E. Coli | ≤2MPN/g | N.D. |
| Salmonella | N.D. | N.D. |
| Ethanol (by GC) | ≤5000ppm | 200ppm |
| Storage | -80°C, 2 years; -20°C, 1 year (Sealed storage, away from moisture) | |
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| Shaanxi Chuzhan is a technology enterprise specializing in the research and development, production of chemicals and equipment customization services, providing OEM/ODM full-chain solutions. We offer flexible full-process customized services, from formula research and development to equipment selection, all can be deeply adapted according to customer requirements. Support full-cycle technical collaboration from small-scale trials, medium-scale trials to large-scale production, equipped with a professional engineering team to provide process optimization suggestions, and can customize packaging labels according to the brand requirements of customers. | ||
Pharmacokinetics
Tiamulin is administered orally, primarily via feed or water medication. Its bioavailability varies depending on the formulation and route of administration. In pigs, oral bioavailability ranges from 40% to 60%, with peak plasma concentrations achieved within 2–4 hours. The drug is extensively metabolized in the liver and excreted primarily in the feces, with minimal renal excretion.
Tissue Distribution
It distributes widely throughout the body, with high concentrations in the lungs, liver, and intestinal tissues. This distribution profile is particularly advantageous in treating respiratory and enteric infections. In pigs, lung concentrations can exceed plasma levels by 5–10 times, ensuring effective therapy against respiratory pathogens.
Elimination Half-Life
The elimination half-life of Tiamulin in pigs is approximately 4–6 hours, necessitating twice-daily dosing for most indications. However, its prolonged retention in tissues extends its therapeutic effect beyond the plasma half-life, allowing for less frequent administration in some cases.
How Tiamolin Affects Bacterial Protein Synthesis
Tiamulin (thiamutilin) plays a key role as an important antibiotic against specific bacterial infections in veterinary and some human medicine. The core mechanism of its antimicrobial action is the interference with bacterial protein synthesis:
Binding to the 50S subunit of the ribosome
Bacterial protein synthesis takes place mainly on the ribosome, which consists of a large subunit (50S) and a small subunit (30S).The main target of thiamutilin's action is the 50S subunit of the bacterial ribosome. When thiamutilin enters the bacterial cell, it specifically binds to the 50S subunit. This binding has a high affinity and specificity, and can accurately recognize and bind to a specific region of the 50S subunit, which plays a key role in protein synthesis, including catalyzing the formation of peptide bonds, and the binding of thiamutilin to this subunit lays the groundwork for subsequent interference with protein synthesis.
Obstruction of peptidyltransferase activity
During protein synthesis, peptidyltransferase is a key enzyme that catalyzes the formation of peptide bonds, and it is located in the peptidyltransferase active center (PTC) of the 50S subunit of the ribosome.The binding of thiamutilin to the 50S subunit will directly act on the peptidyltransferase active center. It alters the spatial conformation of the active center by occupying the key site of the active center, thus hindering the normal function of peptidyl transferase. The inability of peptide acyltransferase to function properly prevents it from catalyzing the formation of peptide bonds, resulting in a blockage of the peptide chain elongation process.
Interference with tRNA binding to ribosomes
During protein synthesis, transfer RNAs (tRNAs) play a role in carrying amino acids and transporting them to the appropriate site on the ribosome. tRNAs have specific binding sites on the ribosome, including the A site (aminoacyl site) and the P site (peptide acyl site). tRNAs have a specific binding site to the 50S subunit that overlaps with the tRNAase substrate binding site. binding site overlaps with the tRNAase substrate. This overlap prevents the tRNA from binding properly to the A-site and P-site of the ribosome. When the tRNA cannot bind to the ribosome successfully, amino acids cannot be added to the peptide chain being synthesized in the exact order of the genetic code on the mRNA, further disrupting the normal flow of protein synthesis.
Inhibition of Peptide Chain Elongation and Protein Synthesis Initiation
The process of peptide chain elongation cannot proceed smoothly because thiamutilin hinders peptidyltransferase activity and the binding of tRNA to the ribosome. New amino acids cannot be added to the peptide chain, resulting in an inability to increase the length of the peptide chain and protein synthesis cannot be completed. In addition, Thiamutilin may also have some effect on the initiation phase of protein synthesis. Although its main direct effect is in the peptide chain extension stage, the overall disruption of ribosome function may indirectly interfere with the formation of the initiation complex, causing the initiation process of protein synthesis to be inhibited to a certain extent as well.
Antibacterial effect embodied
Thiamutilin comprehensively interferes with the process of bacterial protein synthesis through a series of mechanisms of action mentioned above. Since proteins are essential for bacterial growth, reproduction and maintenance of life activities, the inhibition of protein synthesis will lead to the inhibition of bacterial growth and reproduction. At low concentration, thiamutilin mainly shows its inhibitory effect, slowing down or stopping the growth of bacteria; while at high concentration, it can further destroy the physiological function of bacteria, leading to the death of bacteria, thus exerting its bactericidal effect.
In summary, thiamutilin affects the protein synthesis of bacteria by binding to the 50S subunit of bacterial ribosomes, interfering with peptidyltransferase activity, binding of tRNA to ribosomes, inhibiting peptide chain extension and protein synthesis initiation, etc., and then achieves antibacterial effect. This unique antimicrobial mechanism makes thiamutilin important in the fight against specific bacterial infections.
Resistance and Stewardship
Mechanisms of Resistance
Resistance to thiamutilin is primarily mediated by mutations in the 23S rRNA gene, which alter the binding site of the antibiotic. Additionally, efflux pumps and enzymatic inactivation may contribute to resistance, although these mechanisms are less common. The emergence of Tiamulin-resistant strains of M. hyopneumoniae and B. hyodysenteriae has been reported, particularly in regions with intensive antibiotic use.
Stewardship Measures
To mitigate the development of resistance, veterinarians and producers should adopt antibiotic stewardship practices, including:
Rotating antibiotics with different mechanisms of action.
Using narrow-spectrum antibiotics whenever possible.
Implementing vaccination programs to reduce the need for antibiotic treatments.
Monitoring resistance patterns through surveillance programs.
Future Directions and Research Needs
Novel Formulations and Delivery Systems
Research is underway to develop sustained-release formulations of Tiamulin, aiming to extend its duration of action and reduce the frequency of administrations. Nanoparticle-based delivery systems may enhance its tissue penetration and bioavailability, particularly in hard-to-reach infections. Additionally, topical formulations for dermatological conditions in pigs could expand its clinical applications.
Combination Therapies
Combining Tiamulin with other antimicrobials or immunomodulators could enhance its efficacy against resistant pathogens or mixed infections. For example, pairing it with a beta-lactam antibiotic may provide synergistic activity against Staphylococcus aureus. Additionally, combining it with non-steroidal anti-inflammatory drugs (NSAIDs) could reduce inflammation and improve clinical outcomes in severe respiratory cases.
Surveillance and Resistance Management
The emergence of resistance to Tiamulin underscores the need for ongoing surveillance. National and international networks should monitor resistance patterns and guide treatment decisions. Additionally, research into alternative targets or combination therapies could help mitigate resistance development.
Expansion of Indications
While Tiamulin is primarily used in pigs and poultry, its efficacy against other pathogens and species warrants further exploration. For example, its activity against Mycoplasma bovis suggests potential for use in cattle with respiratory disease. Additionally, its efficacy against certain Gram-positive bacteria may make it valuable in treating mastitis in dairy cows.
Tiamulin remains a critical tool in veterinary medicine, offering a unique mechanism of action, broad-spectrum antimicrobial activity, and favorable pharmacokinetic properties. Its efficacy in treating respiratory and enteric diseases in pigs and poultry has made it indispensable in modern livestock production. However, the emergence of resistance and the need for prudent use highlight the importance of ongoing research and surveillance. As the livestock industry continues to evolve, Tiamulin will remain a vital component of animal health management, ensuring the welfare of livestock and the sustainability of food production. Future research should focus on optimizing its use, exploring novel formulations, and addressing emerging resistance challenges to sustain its efficacy for generations to come.
By adhering to responsible use guidelines and investing in research and development, the veterinary community can ensure that Tiamulin continues to play a pivotal role in safeguarding animal health and supporting global food security.
Immunosuppression
In severe bacterial infections, excessive inflammatory responses (such as sepsis) may lead to multiple organ failure. Tylosin can inhibit the excessive secretion of inflammatory factors through the following pathways:
Blocking the NF-κB signaling pathway: Tiamulin can inhibit the activity of IκB kinase (IKK) and reduce the nuclear translocation of NF-κB, thereby decreasing the transcription of pro-inflammatory factors such as TNF-α and IL-6.
For instance, in a model of Actinobacillus pleuropneumoniae infection in pigs, the level of TNF-α in the bronchoalveolar lavage fluid of the tiamulin-treated group decreased by 65% compared to the infected control group. Promoting the release of anti-inflammatory factors: Tiamulin can upregulate the secretion of IL-10 by macrophages, inhibiting inflammatory responses through a negative feedback mechanism. Experiments have shown that the supernatant of macrophages treated with tiamulin can reduce the ability of T cells to secrete IFN-γ by 30%, while the level of IL-10 increases twofold.
Clinical case: In a severe case of porcine dysentery, the combination therapy of tiamulin and dexamethasone controlled diarrhea symptoms earlier than the group treated with dexamethasone alone, and the recurrence rate was reduced by 50%, suggesting that the immunosuppressive effect of tiamulin is targeted.
Regulating immune cell metabolism
Excessive inflammatory response is often accompanied by metabolic disorders in immune cells (such as hyperglycolysis and mitochondrial dysfunction). Tylosin can restore the metabolic homeostasis of immune cells through the following mechanisms:
Enhancing mitochondrial biogenesis: Tylosin can upregulate the expression of mitochondrial transcription factor A (TFAM) in macrophages, promote mitochondrial DNA replication, and increase ATP production.
For example, in an in vitro inflammation model, the mitochondrial membrane potential of macrophages in the Tylosin-treated group was 25% higher than that in the control group, and the oxygen consumption rate increased by 30%. Inhibiting metabolic reprogramming: Tiamulin can block the accumulation of HIF-1α (hypoxia-inducible factor-1α) and prevent excessive polarization of macrophages towards the pro-inflammatory (M1) phenotype. Experiments have shown that macrophages treated with tiamulin secrete 40% less NO compared to the control group, without significant decrease in phagocytic ability.
Less popular significance: This mechanism provides a new approach for treating inflammatory diseases (such as autoimmune diseases), which achieves safer immune regulation by regulating the metabolism of immune cells rather than directly inhibiting immune response.
Frequently Asked Questions
Is tiamulin bactericidal or bacteriostatic?
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bacteriostatic
Tiamulin demonstrates a bacteriostatic mechanism of action, by obstructing the 50S ribosomal subunit within bacteria, thereby inhibiting the peptidyl transferase enzyme.
What are the side effects of the drug tiamulin?
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Adverse Reactions
Overdoses of tiamulin have sometimes produced transitory salivation, vomiting and an apparent calming effect on pigs. In rare cases, redness of the skin, primarily over the ham and underline, has been observed during medication.
What is tiamulin used for?
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Tiamulin is a semi-synthetic antibiotic belonging to the pleuromutilin group of antibiotics and it is used only in veterinary medicine. Tiamulin is used for the treatment and prevention of gastrointestinal and respiratory infections caused by different bacterial pathogens in pigs, poultry and rabbits.
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