Tylvalosin Tartrate (cas 63428-13-7)
Tylosin 3-acetate 4B-(3-methylbutanoate) (2R,3R)-2,3-dihydroxybutanedioate Comprehensive Information Table
| Category | Details |
|---|---|
| CAS Number | 63428-13-7 |
| Synonyms | Aivlosin Tartrate, Tylvalosin Tartrate, Acetylisovaleryltylosin Tartrate, Tylosin 3-acetate 4B-(3-methylbutanoate) |
| Chemical Formula | C₅₇H₉₃NO₂₅ |
| Molecular Weight | 1192.34 g/mol |
| EINECS Number | 256-145-7 |
| Melting Point | 208–211°C |
| Solubility | Slightly soluble in DMSO and methanol; practically insoluble in water |
| Appearance | White to off-white powder |
| Stability | Hygroscopic; requires inert atmosphere and storage at -20°C |
| Optical Activity | [α]²⁵/D +54° (c = 2 in H₂O) |
| Bulk Density | ~640 kg/m³ |
| Refractive Index | 1.56 (C=10, H₂O) |
Key Applications & Pharmacological Properties
- Veterinary Medicine:
- Antibacterial Agent: Broad-spectrum activity against Gram-positive and Gram-negative bacteria, including Mycoplasma and Lawsonia intracellularis 3.
- Anti-protozoal: Controls Eimeria infections in poultry.
- Immunomodulatory: Enhances macrophage activity against viral infections (e.g., porcine reproductive and respiratory syndrome virus, PRRSV) 3.
- Key Mechanisms:
- Inhibits bacterial protein synthesis by binding to the 50S ribosomal subunit.
- Modulates host immune responses by enhancing phagocytosis and cytokine production.
- Clinical Uses:
- Swine: Treats Mycoplasma pneumonia and Salmonella infections; reduces post-weaning diarrhea.
- Poultry: Controls cecal coccidiosis and respiratory diseases.
- Cattle: Addresses mastitis and metritis caused by Staphylococcus and Streptococcus spp.
Synthesis & Production
- Fermentation-Based Production:
- Produced via bioconversion of tylosin using Streptomyces strains (e.g., S. fradiae) with acetylation and isovaleryl group introduction 3.
- Key steps:
- Acetylation: Introduction of 3-O-acetyl group.
- Isovaleroylation: Attachment of 4”-O-isovaleryl group.
- Salt Formation: Reacting with (2R,3R)-2,3-dihydroxybutanedioic acid to form tartrate salt.
- Optimization Strategies:
- Strain improvement (e.g., UV mutagenesis of S. fradiae YN554) to enhance yield 3.
- Downstream purification via crystallization and chromatography.
Quality Control & Safety
| Parameter | Specifications |
|---|---|
| Purity | ≥98% (HPLC) |
| Impurities | ≤0.5% total organic impurities |
| Heavy Metals | ≤10 ppm (Pb, Cd, Hg) |
| Toxicity | – LD₅₀ (mouse): >5000 mg/kg (oral) – Acute Toxicity: Low in mammals |
| Handling Precautions | Wear gloves/face shields; avoid inhalation. Store under inert atmosphere. |
Regulatory Status
- Approved Uses:
- Veterinary: Authorized for swine, poultry, and cattle in the EU and China.
- Human Use: Not approved; restricted to animal therapeutic applications.
- Restrictions:
- Banned in aquaculture and pet food in the EU due to residue concerns.
- Subject to withdrawal periods (e.g., 14 days for swine, 5 days for poultry).
Research & Development
- Novel Formulations:
- Controlled-Release Pellets: Improve bioavailability in ruminants.
- Nanoparticle Suspensions: Enhanced delivery for intramammary infections.
- Combination Therapies:
- Synergistic effects with tetracyclines against multi-drug resistant Mycoplasma.
For detailed toxicology data or synthesis protocols, consult regulatory databases (e.g., FDA, EMA) or specialized pharmacological references.
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