The primary target of Tylosin tartrate is the bacterial ribosome, specifically the 50S subunit (L27 protein), where it inhibits protein synthesis. By binding to the 50S ribosomal subunit, Tylosin tartrate blocks the elongation of peptide chains during translation, thereby exerting its bacteriostatic effect. The compound has a broad spectrum of activity against Gram-positive bacteria and mycoplasma, but it has much less activity against most Gram-negative bacteria and fungi. The selectivity of Tylosin tartrate for Gram-positive bacteria is related to the differences in cell wall structure and ribosome composition between Gram-positive and Gram-negative organisms. The compound's activity against mycoplasmas, which lack a cell wall, is particularly noteworthy and makes it a key antibiotic for controlling mycoplasmosis in poultry. Tylosin tartrate is also effective against certain Gram-negative bacteria, although its spectrum is limited. The compound's mechanism of action is similar to that of other macrolide antibiotics, such as erythromycin and azithromycin, which also bind to the 50S ribosomal subunit. However, Tylosin tartrate has a distinct binding site and may have a different spectrum of activity compared to other macrolides. The compound's bacteriostatic activity is concentration-dependent, and it is typically used at doses that achieve inhibitory concentrations in target tissues. Resistance to Tylosin tartrate can occur through various mechanisms, including ribosomal mutations, efflux pumps, and enzymatic inactivation. Monitoring of resistance patterns is important for maintaining the efficacy of the compound in veterinary practice. The compound's target specificity and its effectiveness against key veterinary pathogens make it an important tool for animal health and disease management.

By attaching itself to the 23S rRNA of the 50S subunit of bacterial ribosomes, tylosin tartrate binds to bacteria and has antibacterial properties [1]. Additionally, Gram-negative bacteria of Mycobacterium haemolyticus 11935, Pseudomonas multocida 4407, and E. coli are inhibited from growing by tylosin tartrate. bacteria ATCC 25922 and E. coli AS19rlmAI, in that order [3].
In vitro, Tylosin tartrate exhibits potent antimicrobial activity against a wide range of bacterial pathogens, particularly Gram-positive organisms and mycoplasmas. The compound is highly effective against Mycoplasma species, including Mycoplasma gallisepticum and Mycoplasma synoviae, which are important pathogens in poultry. It also shows good activity against Gram-positive bacteria such as Staphylococcus aureus, Streptococcus species, and Clostridium species. The compound's activity against Gram-negative bacteria is more limited, but it may be effective against some species, particularly at higher concentrations. The minimum inhibitory concentrations (MICs) of Tylosin tartrate against various bacterial strains are determined using standard broth microdilution or agar diffusion methods following CLSI guidelines. The compound's bacteriostatic activity is concentration-dependent, and its efficacy is influenced by factors such as pH, inoculum size, and the presence of serum. In addition to its direct antimicrobial activity, Tylosin tartrate may also have immunomodulatory effects that contribute to its therapeutic efficacy. The compound's in vitro activity is well-characterized and forms the basis for its use in veterinary medicine. However, the emergence of resistance to macrolide antibiotics, including Tylosin, has been reported, and susceptibility testing is recommended to guide the appropriate use of the compound. The in vitro activity data are also used to establish clinical breakpoints for susceptibility testing and to monitor resistance trends in veterinary pathogens.

In rats treated with lipopolysaccharide (LPS), tylosin tartrate (10–500 mg/kg; subcutaneous injection) typically lowers increased TNF-α and IL-1β levels and enhances IL-10 levels [4].
In vivo, Tylosin tartrate is effective against a range of bacterial infections in livestock and poultry, including bacterial dysentery, respiratory diseases, and mycoplasmosis. The compound is administered orally as a feed additive or via drinking water, and it is well-absorbed from the gastrointestinal tract. It is distributed to various tissues, including the respiratory tract, where it reaches therapeutic concentrations. In poultry, Tylosin tartrate is used to control Mycoplasma infections, which can cause significant economic losses due to reduced growth, egg production, and increased mortality. In swine and cattle, the compound is used to treat bacterial dysentery and respiratory diseases, including those caused by Pasteurella, Streptococcus, and other pathogens. The compound's efficacy in vivo is influenced by factors such as the dose, route of administration, and the susceptibility of the target pathogen. The compound is also used as a feed additive for growth promotion, although this use is increasingly regulated due to concerns about antibiotic resistance. The in vivo efficacy of Tylosin tartrate has been well-established through extensive clinical use and controlled studies in target animal species. The compound's safety and efficacy profiles are well-characterized, and it is an important tool for maintaining animal health and productivity in veterinary practice. However, the emergence of resistance and the potential for residues in food products necessitate careful use and adherence to withdrawal periods.

In vitro antimicrobial activity of Tylosin tartrate is evaluated using standard broth microdilution or agar diffusion methods against various bacterial strains. For broth microdilution assays, serial two-fold dilutions of Tylosin tartrate are prepared in appropriate growth medium in 96-well plates. Bacterial suspensions are added to each well, and the plates are incubated overnight at 37°C. The minimum inhibitory concentration (MIC) is determined as the lowest concentration of the compound that inhibits visible bacterial growth. For agar diffusion assays, filter paper disks impregnated with Tylosin tartrate are placed on agar plates inoculated with the test organism. After incubation, the diameter of the inhibition zone is measured, and the results are interpreted based on established criteria. The in vitro activity against Mycoplasma species is assessed using specialized culture media and incubation conditions, as mycoplasmas have specific growth requirements. The MIC values obtained from these assays are used to determine the susceptibility of bacterial isolates to Tylosin tartrate and to monitor resistance trends. The compound's activity may be affected by various factors, including the pH of the medium, the presence of serum, and the inoculum size. Quality control strains with known MIC ranges are included in each assay to ensure the validity of the results. The in vitro activity data are also used to establish clinical breakpoints for susceptibility testing and to guide the appropriate use of the compound in veterinary practice.

In vitro cellular assays for Tylosin tartrate are typically performed using bacterial cell cultures. The compound's antimicrobial activity is assessed by measuring its ability to inhibit bacterial growth. Broth microdilution assays are performed in 96-well plates with serial dilutions of Tylosin tartrate. Bacterial growth is measured by optical density at 600 nm after overnight incubation to determine MIC values. The compound's bacteriostatic activity is concentration-dependent, and its efficacy is influenced by factors such as pH, inoculum size, and the presence of serum. In addition to MIC determination, the compound's effects on bacterial protein synthesis can be assessed using radioisotopic labeling or other methods to measure the incorporation of amino acids into proteins. The compound's effects on bacterial cell morphology and ultrastructure can be examined using electron microscopy. The in vitro activity against Mycoplasma species is assessed using specialized culture media and incubation conditions, as mycoplasmas have specific growth requirements. The compound's activity against intracellular bacteria, such as certain Mycoplasma species, may also be assessed using cell culture models where bacteria are grown inside host cells. These cellular assays are essential for characterizing the antimicrobial activity of Tylosin tartrate and for understanding its mechanism of action. The results of these assays provide valuable information for the clinical use of the compound and for monitoring resistance patterns.

Animal/Disease Models: balb/c (Bagg ALBino) mouse (2-3 months old, 20-25 g) [4]
Doses: 10 mg/kg, 100 mg/kg, 500 mg/kg
Route of Administration: subcutaneous injection
Experimental Results: diminished increase In mice treated with TNF-α LPS (250 µg), IL-1β and IL-1β levels were elevated, but IL-10 levels were increased.
In vivo efficacy studies of Tylosin tartrate are conducted in poultry, swine, or cattle models infected with Mycoplasma or pathogenic bacteria. In these studies, animals are infected with the target pathogen, and then treated with Tylosin tartrate via the intended route of administration (e.g., feed, water, or injection). Clinical signs, mortality, bacterial load, and histopathological changes are monitored to assess the compound's efficacy. In poultry, the compound is evaluated for its ability to control Mycoplasma infections, which can cause respiratory disease, reduced growth, and egg production losses. In swine and cattle, the compound is evaluated for its efficacy against bacterial dysentery and respiratory diseases. The studies are typically conducted under controlled conditions, and the results are used to establish the optimal dose and treatment regimen for the compound. The compound's safety and efficacy profiles are well-characterized, and it is an important tool for maintaining animal health and productivity in veterinary practice. In addition to therapeutic studies, the compound is also evaluated for its use as a feed additive for growth promotion, although this use is increasingly regulated due to concerns about antibiotic resistance. The in vivo efficacy data are essential for regulatory approval and for guiding the appropriate use of the compound in veterinary medicine.

Following oral administration, Tylosin tartrate is absorbed from the gastrointestinal tract and distributed to various tissues. The compound is metabolized in the liver and excreted primarily in bile and urine. Pharmacokinetic parameters including Cmax, Tmax, half-life, and bioavailability are determined in target animal species to guide dosing regimens. The compound's distribution to tissues, including the respiratory tract, is important for its efficacy against respiratory pathogens. The compound's bioavailability may be influenced by factors such as the formulation, the presence of food, and the animal species. The compound is also used in research focused on veterinary medicine, serving as a model compound in drug formulation studies to help researchers understand the pharmacokinetics and efficacy of similar antibiotics. The pharmacokinetic data obtained from these studies are essential for designing appropriate dosing regimens and for interpreting the results of efficacy and toxicity studies. The compound's metabolism and clearance pathways are also characterized to understand its elimination from the body. Withdrawal periods are established based on the compound's pharmacokinetics and tissue residue depletion studies to ensure food safety.

Toxicological studies in animals have established the safety profile of Tylosin tartrate for veterinary use. The compound is generally well-tolerated at therapeutic doses, but adverse effects may include gastrointestinal disturbances at high doses. The compound is contraindicated in horses and other species with sensitive gastrointestinal flora, as it can cause severe diarrhea and colitis. Withdrawal periods are established to ensure food safety and to prevent residues in meat, milk, and eggs. The compound's toxicity is low in target animal species, but it may be toxic to certain non-target species, such as horses. In addition to its direct toxicity, the use of Tylosin tartrate as a feed additive has raised concerns about the selection of antibiotic-resistant bacteria, and its use is increasingly regulated. The compound's safety and efficacy profiles are well-characterized, and it is an important tool for maintaining animal health and productivity in veterinary practice. The compound is also used in research focused on veterinary medicine, serving as a model compound in drug formulation studies to help researchers understand the pharmacokinetics and efficacy of similar antibiotics. Researchers must carefully consider the potential for adverse effects and the emergence of resistance when using Tylosin tartrate in experimental studies. The compound is intended for veterinary use only and is not approved for human therapeutic use. Standard safety precautions should be followed when handling Tylosin tartrate, including the use of appropriate personal protective equipment and adherence to institutional safety guidelines.

[1]. Resistance to the macrolide antibiotic tylosin is conferred by single methylations at 23S rRNA nucleotides G748 and A2058 acting in synergy. Proc Natl Acad Sci U S A. 2002 Nov 12; 99(23): 14658–14663.

[2]. In Vitro Evaluation of the Effects of Tylosin on the Composition and Metabolism of Canine Fecal Microbiota. Animals (Basel). 2020 Jan; 10(1): 98.

[3]. Inhibition of Protein Synthesis on the Ribosome by Tildipirosin Compared with Other Veterinary Macrolides. Antimicrob Agents Chemother. 2012 Nov; 56(11): 6033–6036.

[4]. Effects of tylosin on serum cytokine levels in healthy and lipopolysaccharide-treated mice. Acta Vet Hung. 2010 Mar;58(1):75-81.

macrolide antibiotic extracted from Streptomyces freundii cultures. This drug is effective against various microorganisms in animals but ineffective against humans.
See also: Tylosin (contains the active ingredient); estradiol; trenbolone acetate; tylosin tartrate (one of the ingredients); estradiol benzoate; progesterone; tylosin tartrate (one of the ingredients)...See more...
Tylosin tartrate (CAS 74610-55-2) is a veterinary antibiotic widely used as a feed additive for promoting animal growth and for treating bacterial dysentery and respiratory diseases in poultry, swine, and cattle. It is a macrolide antibiotic derived from Streptomyces fradiae that inhibits bacterial protein synthesis by binding to the 50S ribosomal subunit. The compound exhibits a broad spectrum of activity against Gram-positive organisms and mycoplasma, with limited activity against Gram-negative organisms. Tylosin tartrate is particularly effective against mycoplasmas, making it a key antibiotic for controlling mycoplasmosis in poultry. It is also used in aquaculture and apiculture. The compound is commonly used in veterinary medicine for the treatment and control of diseases caused by susceptible bacteria, particularly in livestock and poultry. Its use as a feed additive has been widespread in the livestock industry for growth promotion and disease prevention. The compound is also utilized in research focused on veterinary medicine, serving as a model compound in drug formulation studies to help researchers understand the pharmacokinetics and efficacy of similar antibiotics. Tylosin tartrate is available as a research-grade standard for analytical and formulation studies, and its safety and efficacy have been well-established in veterinary practice. Despite its widespread use, resistance to macrolide antibiotics, including Tylosin, has been reported and should be monitored in veterinary and agricultural settings. The compound is not approved for human therapeutic use and is intended for veterinary applications only. When handling Tylosin tartrate, researchers should follow standard safety protocols for handling chemical reagents, including the use of appropriate personal protective equipment and working in a well-ventilated area.

C50H83NO23

1066.1869

1065.535

74610-55-2

Tylosin;1401-69-0;Tylosin phosphate;1405-53-4

60196281

White to off-white solid powder

128 - 132ºC

9

24

16

74

1700

23

CC[C@@H]1[C@H](/C=C(/C=C/C(=O)[C@@H](C[C@@H]([C@@H]([C@H]([C@@H](CC(=O)O1)O)C)O[C@H]2[C@@H]([C@H]([C@@H]([C@H](O2)C)O[C@H]3C[C@@]([C@H]([C@@H](O3)C)O)(C)O)N(C)C)O)CC=O)C)\C)CO[C@H]4[C@@H]([C@@H]([C@@H]([C@H](O4)C)O)OC)OC.[C@@H]([C@H](C(=O)O)O)(C(=O)O)O

ICVKYYINQHWDLM-KBEWXLTPSA-N

InChI=1S/C46H77NO17.C4H6O6/c1-13-33-30(22-58-45-42(57-12)41(56-11)37(52)26(5)60-45)18-23(2)14-15-31(49)24(3)19-29(16-17-48)39(25(4)32(50)20-34(51)62-33)64-44-38(53)36(47(9)10)40(27(6)61-44)63-35-21-46(8,55)43(54)28(7)59-35;5-1(3(7)8)2(6)4(9)10/h14-15,17-18,24-30,32-33,35-45,50,52-55H,13,16,19-22H2,1-12H3;1-2,5-6H,(H,7,8)(H,9,10)/b15-14+,23-18+;/t24-,25+,26-,27-,28+,29+,30-,32-,33-,35+,36-,37-,38-,39-,40-,41-,42-,43+,44+,45-,46-;1-,2-/m11/s1

(2R,3R)-2,3-dihydroxybutanedioic acid;2-[(4R,5S,6S,7R,9R,11E,13E,15R,16R)-6-[(2R,3R,4R,5S,6R)-5-[(2S,4R,5S,6S)-4,5-dihydroxy-4,6-dimethyloxan-2-yl]oxy-4-(dimethylamino)-3-hydroxy-6-methyloxan-2-yl]oxy-16-ethyl-4-hydroxy-15-[[(2R,3R,4R,5R,6R)-5-hydroxy-3,4-dimethoxy-6-methyloxan-2-yl]oxymethyl]-5,9,13-trimethyl-2,10-dioxo-1-oxacyclohexadeca-11,13-dien-7-yl]acetaldehyde

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Note: Please store this product in a sealed and protected environment, avoid exposure to moisture.

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

H2O : ≥ 100 mg/mL (~93.79 mM)
DMSO : ≥ 100 mg/mL (~93.79 mM)

Solubility in Formulation 1: ≥ 2.5 mg/mL (2.34 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

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Solubility in Formulation 2: ≥ 2.5 mg/mL (2.34 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

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Solubility in Formulation 3: ≥ 2.5 mg/mL (2.34 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

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Solubility in Formulation 4: 100 mg/mL (93.79 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication.

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 (Please use freshly prepared in vivo formulations for optimal results.)