| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 500mg |
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| Other Sizes |
| Targets |
Bacterial 50S ribosomal subunit. Tylvalosin binds to the 50S ribosomal subunit, specifically to the 23S rRNA, inhibiting bacterial protein synthesis at the translocation step. It is bacteriostatic but has time-dependent antibacterial activity. Additionally, Tylvalosin exerts anti-inflammatory effects by suppressing NF-kappaB activation, reducing pro-inflammatory cytokine production (e.g., TNF-alpha, IL-1beta, IL-6).
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| ln Vitro |
In vitro, Tylvalosin exhibits potent antibacterial activity against Gram-positive bacteria, including Mycoplasma species, Lawsonia intracellularis, and various respiratory pathogens (e.g., Streptococcus suis, Pasteurella multocida). MIC values against M. hyopneumoniae and M. gallisepticum are typically ≤0.5 ug/mL. It also shows activity against Brachyspira hyodysenteriae. The anti-inflammatory activity has been demonstrated in cell-based assays.
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| ln Vivo |
Tylvalosin tartrate, administered orally via drinking water or feed at 10-20 mg/kg body weight per day for 7-14 days, effectively treats respiratory disease in pigs and poultry. In pigs, it reduces clinical signs of enzootic pneumonia and proliferative enteropathy, improves weight gain, and reduces lung lesion scores. In poultry, it is effective against Mycoplasma gallisepticum infections. It also exhibits anti-inflammatory effects in various models, attenuating acute lung injury.
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| Enzyme Assay |
Not applicable. The mechanism of action involves ribosomal binding, but direct cell-free assays are not commonly reported. For evaluation of anti-inflammatory effects in cell-free systems, NF-kappaB DNA-binding activity can be measured. Nuclear extracts are incubated with Tylvalosin (0.1-100 uM) and a biotinylated NF-kappaB probe for 30 minutes. The DNA-protein complex is detected by EMSA. However, such assays are not standard for this compound.
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| Cell Assay |
Tylvalosin has been shown to inhibit LPS-induced NO production in RAW264.7 macrophages. For anti-inflammatory studies, RAW264.7 macrophages are seeded in 96-well plates at 1×10⁵ cells/well and stimulated with LPS (1 ug/mL) in the presence or absence of Tylvalosin (0.1-100 uM) for 24 hours. NO production is measured by Griess reaction, and TNF-alpha, IL-6, and IL-1beta levels in culture supernatant are quantified by ELISA. NF-kappaB p65 translocation is examined by immunofluorescence. For anti-mycoplasma activity, M. hyopneumoniae cultures are seeded in 96-well plates and treated with Tylvalosin (0.001-100 ug/mL) for 48-72 hours. MIC is determined by colorimetric method using a tetrazolium dye.
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| Animal Protocol |
In a porcine enzootic pneumonia model, weanling pigs (4-6 weeks old) are challenged intratracheally with M. hyopneumoniae (10⁶-10⁷ CCU). When clinical signs develop (2-4 weeks post-challenge), Tylvalosin tartrate is administered orally via feed or drinking water at a dose of 10-20 mg/kg body weight daily for 7-14 days. Clinical respiratory scores, rectal temperatures, and body weights are recorded every 2-3 days. At necropsy, lung lesion scores are evaluated macroscopically, and lung tissue samples are collected for histopathology and mycoplasma re-isolation. In a proliferative enteropathy model, pigs are challenged orally with L. intracellularis and treated similarly. Efficacy is measured by reduction of diarrhea, improved weight gain, and reduced L. intracellularis shedding in feces by PCR.
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| ADME/Pharmacokinetics |
In pigs, Tylvalosin is well absorbed after oral administration, with peak plasma concentrations reached within 2-4 hours. The bioavailability is moderate (approximately 30-50%) due to first-pass metabolism. It is widely distributed to tissues, particularly lung and intestinal mucosa, with tissue concentrations exceeding plasma levels. The elimination half-life is approximately 6-12 hours. It is metabolized in the liver, primarily via demethylation and desosamine sugar cleavage. In poultry, absorption is also effective, and it is detected in lung tissue for extended periods (up to 72 hours).
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| Toxicity/Toxicokinetics |
Tylvalosin has a favorable safety profile in target species at therapeutic doses (10-20 mg/kg). Mild, transient diarrhea may occur in some pigs. In chronic toxicity studies, no significant adverse effects were observed. The compound is not known to be genotoxic or carcinogenic. In humans, Tylvalosin is not approved for use, and limited toxicity data is available. Standard safety precautions should be used when handling.
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| References |
[1]. Albert Philip Adrian Mockett, et al. Use of tylvalosin as antiviral agent. Patent. WO2008007104. [2]. Zhao Z, et al. Tylvalosin exhibits anti-inflammatory property and attenuates acute lung injury in different models possibly through suppression of NF-κB activation. Biochem Pharmacol. 2014 Jul 1;90(1):73-87.
[3]. Moges R, et al. Anti-Inflammatory Benefits of Antibiotics: Tylvalosin Induces Apoptosis of Porcine Neutrophils and Macrophages, Promotes Efferocytosis, and Inhibits Pro-Inflammatory CXCL-8, IL1α, and LTB4 Production, While Inducing the Release of Pro-Resolving Lipoxin A4 and Resolvin D1. Front Vet Sci. 2018 Apr 11;5:57. |
| Additional Infomation |
See also: Tylvalosin tartrate (active ingredient).
Drug Indications Swine: Treatment and prevention of endemic pneumonia in pigs; treatment of proliferative enteritis (ileitis) in pigs; treatment and prevention of swine dysentery. Chickens: Treatment and prevention of respiratory diseases caused by Mycoplasma gallisepticum. Pheasants: Treatment of respiratory diseases caused by Mycoplasma gallisepticum. Turkeys: Treatment of respiratory diseases in turkeys caused by Ornithobacterium avium susceptible to Tylvalosin. Tylvalosin is also known as Acetylisovaleryltylosin. The molecular formula is C53H87NO19, and the molecular weight is 1042.25. It is a 16-membered semi-synthetic macrolide antibiotic. It is formulated as a premix (Aivlosin®) for feed administration or as a water-soluble powder for drinking water treatment. It is a prescription-only veterinary drug. It is not approved for human use. IUPAC name: [(2S,3S,4R,6S)-6-[(2R,3S,4S,5R,6R)-4-[(2R,3S,4R,5R,6S)-4,5-dihydroxy-6-methyloxan-2-yl]oxy-2-hydroxy-5-[(2S,3R,4S,5R,6R)-5-hydroxy-3,4-dimethoxy-6-methyloxan-2-yl]oxy-3-methyloxan-6-yl]-4-hydroxy-2-methylcyclohexyl] 3-methylbutanoate. |
| Molecular Formula |
C53H87NO19
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|---|---|
| Molecular Weight |
1042.25
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| Exact Mass |
1041.59
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| CAS # |
63409-12-1
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| Related CAS # |
Tylvalosin tartrate;63428-13-7;Tylvalosin-d9
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| PubChem CID |
6441094
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| Appearance |
White to off-white solid powder
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| Density |
1.21g/cm3
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| Boiling Point |
1005.4ºC at 760 mmHg
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| Melting Point |
>105°C (dec.)
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| Flash Point |
561.8ºC
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| Index of Refraction |
1.534
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| LogP |
4.001
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
20
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| Rotatable Bond Count |
19
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| Heavy Atom Count |
73
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| Complexity |
1860
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| Defined Atom Stereocenter Count |
21
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| SMILES |
CC(CC(O[C@H]1[C@H](C)O[C@@H](O[C@@H]2[C@@H](C)O[C@H](O[C@@H]3[C@@H](CC=O)C[C@@H](C)C(=O)C=CC(C)=C[C@H](CO[C@@H]4O[C@H](C)[C@@H](O)[C@@H](OC)[C@H]4OC)[C@@H](CC)OC(=O)C[C@@H](OC(=O)C)[C@@H]3C)[C@H](O)[C@@H]2N(C)C)C[C@@]1(C)O)=O)C |c:30,t:27,&1:5,6,9,11,12,15,17,18,23,32,35,37,39,41,44,47,54,59,61,63,68|
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| InChi Key |
KCJJINQANFZSAM-HZDSEHBESA-N
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| InChi Code |
InChI=1S/C53H87NO19/c1-16-38-36(26-65-52-49(64-15)48(63-14)44(60)31(7)67-52)22-28(4)17-18-37(57)29(5)23-35(19-20-55)46(30(6)39(69-34(10)56)24-41(59)70-38)73-51-45(61)43(54(12)13)47(32(8)68-51)72-42-25-53(11,62)50(33(9)66-42)71-40(58)21-27(2)3/h17-18,20,22,27,29-33,35-36,38-39,42-52,60-62H,16,19,21,23-26H2,1-15H3/b18-17+,28-22+/t29-,30+,31-,32-,33+,35+,36-,38-,39-,42+,43-,44-,45-,46-,47-,48-,49-,50+,51+,52-,53-/m1/s1
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| Chemical Name |
[(2S,3S,4R,6S)-6-[(2R,3S,4R,5R,6R)-6-[[(4R,5S,6S,7R,9R,11E,13E,15R,16R)-4-acetyloxy-16-ethyl-15-[[(2R,3R,4R,5R,6R)-5-hydroxy-3,4-dimethoxy-6-methyloxan-2-yl]oxymethyl]-5,9,13-trimethyl-2,10-dioxo-7-(2-oxoethyl)-1-oxacyclohexadeca-11,13-dien-6-yl]oxy]-4-(dimethylamino)-5-hydroxy-2-methyloxan-3-yl]oxy-4-hydroxy-2,4-dimethyloxan-3-yl] 3-methylbutanoate
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.9595 mL | 4.7973 mL | 9.5946 mL | |
| 5 mM | 0.1919 mL | 0.9595 mL | 1.9189 mL | |
| 10 mM | 0.0959 mL | 0.4797 mL | 0.9595 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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