CAS
61036-62-2 Purity
95%
61036-62-2 Purity
95%
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Tylvalosin tartrate
CAS
63428-13-7
Catalog Number
ACM63428137-1
Category
Macrocyclic Antibiotics
Molecular Weight
1192.34
Molecular Formula
C57H93NO25
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Specification
Synonyms
Acetylisovaleryltylosin tartrate
Storage
Inert atmosphere, store in freezer, under -20°C
Color
White to light yellow
MDL Number
MFCD31656805
Physical State
Solid
Tylvalosin Tartrate Inhibits PRRSV-Induced Pyroptosis via TLR4/NF-κB Pathway
Zhang, Shi-qin, et al. Journal of Virology (2026): e00202-26.
Tylvalosin tartrate, a third-generation veterinary macrolide antibiotic, has been empirically observed to improve outcomes in pigs affected by porcine reproductive and respiratory syndrome virus (PRRSV). This study elucidated a host-directed mechanism by which tylvalosin tartrate restricts PRRSV replication across diverse lineages.
Experimental Protocol: The in vivo efficacy was evaluated in both naturally and experimentally L1 PRRSV-infected piglets, with tylvalosin tartrate administered at 1,000 mg/kg in feed for 14 days. In vitro experiments were conducted using porcine alveolar macrophages (PAMs) infected with multiple PRRSV-2 lineages (L1, L8.1, L5, and L8.3).
Performance Evaluation: Tylvalosin tartrate treatment significantly reduced serum viremia and inflammatory cytokine levels (IL-1β, IL-6, IL-18) in infected piglets by day 21. Lung histopathology showed markedly improved alveolar integrity and reduced lesion scores. In vitro, 3.125 µM tylvalosin tartrate inhibited replication of all tested PRRSV lineages in PAMs, as confirmed by reduced viral mRNA copies and N protein expression. Transcriptomic data revealed downregulation of pyroptosis-related genes (NLRP3, CASP1, GSDMD). Pretreatment with CASP1 inhibitor VX765 or GSDMD inhibitor LDC7559 similarly impaired PRRSV replication, mirroring the drug's effect. Crucially, tylvalosin tartrate suppressed TLR4 upregulation and NF-κB p65 phosphorylation and nuclear translocation. Both pharmacological inhibition and siRNA knockdown of TLR4 replicated the antiviral and anti-pyroptotic effects, establishing the TLR4/NF-κB/pyroptosis axis as the mechanistic target.
Tylvalosin Tartrate: Transcriptomic Analysis of Anti-PRRSV Gene Regulation
Tang, Xingzhen, et al. Virology Journal 20.1 (2023): 79.
Porcine reproductive and respiratory syndrome (PRRS) remains a major economic threat to the swine industry due to the genetic diversity of PRRSV and the limited cross-protection afforded by current vaccines.
Experimental Protocol: Three commercial tylvalosin tartrate products from different producers (designated Tyl A, Tyl B, and Tyl C) were evaluated using a cell inoculation model. Cytotoxicity was assessed via CCK-8 assay in MARC-145 cells and primary PAMs. Antiviral efficacy was tested against HP-PRRSV strain JXwn06 and NADC30-like strain CHsx1401 using a NanoLuc-tagged recombinant PRRSV reporter virus and immunofluorescence assay. Four treatment regimens (virucidal pre-treatment, pre-inoculation, during-inoculation, and post-inoculation) were compared to identify the effective inhibition stage.
Performance Evaluation: The safe concentration of all three tylvalosin tartrate products was determined as 40 µg/mL in MARC-145 cells. The compounds inhibited PRRSV proliferation in a dose-dependent manner, achieving over 90% reduction at 40 µg/mL. However, they exhibited no direct virucidal effect; sustained presence during the viral proliferation phase was essential for antiviral activity. Both HP-PRRSV and NADC30-like strains were similarly inhibited in MARC-145 cells and PAMs. Transcriptomic analysis identified 16,584 annotated genes, with GO enrichment revealing regulation of signal transduction, proteolysis, and oxidation-reduction processes. KEGG pathway analysis highlighted involvement of PI3K-Akt signaling, FoxO signaling, and ferroptosis pathways. Six antivirus-related genes (HMOX1, ATF3, FTH1, FTL, NR4A1, and CDKN1A) were identified as regulated by tylvalosin tartrate. Western blot confirmed upregulated HMOX1 expression concomitant with PRRSV inhibition, suggesting its contribution to the antiviral mechanism.
Tylvalosin Tartrate Pharmacokinetics in Broiler Chickens After IV and Oral Dosing
Wen, Zeyu, et al. Veterinary Sciences 12.2 (2025): 118.
Tylvalosin is a macrolide antimicrobial used for treating respiratory and enteric bacterial infections in swine and poultry. Forty-eight healthy 5-6-week-old broiler chickens were allocated into intravenous and oral administration groups, each subdivided into three dosage subgroups (5, 10, and 25 mg/kg body weight, n=8 per subgroup). Blood samples were collected at 14 time points from 0 to 24 h post-administration. Plasma concentrations were measured using UPLC-MS/MS with a lower limit of quantification of 1 ng/mL.
Performance Evaluation: Following intravenous administration, the plasma concentration-time curve fitted a two-compartment model, with a rapid distribution half-life of approximately 0.12 h. The elimination half-life ranged from 0.63 to 1.83 h. Following oral administration, the drug was best described by a one-compartment model, reaching peak concentrations within approximately 2-3 h, with Cmax of 287.12 ng/mL at the 25 mg/kg dose. Dose proportionality was absent within the 5-25 mg/kg range for both routes, indicating nonlinear pharmacokinetics attributable to saturation of metabolic enzymes. Absolute oral bioavailability was notably low at 5.92%, 3.56%, and 3.04% for the 5, 10, and 25 mg/kg doses, respectively. Computational simulations demonstrated that a 6-hour dosing interval at 25 mg/kg achieves steady state after the fourth dose, with therapeutic concentrations exceeding the reported MIC against Mycoplasma gallisepticum and Mycoplasma synoviae within 6 h of administration.
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