Manufacturer: Hangzhou Royalchem Co.,LTD.
Website: www.cnroyalchem.com
【 Providing a complete set of intermediates and impurities for Tedizolid 】
【 Providing a complete set of intermediates and impurities for Tedizolid 】
【 Providing a complete set of intermediates and impurities for Tedizolid 】
Here is a detailed product description for Tedizolid Phosphate Disodium Salt (CAS 856867-39-5) :
1. Chemical Identification
Chemical Name: Tedizolid Phosphate Disodium Salt
Synonyms:
TR-701 FA disodium salt
(R)-3-(4-(2-(2-Methyltetrazol-5-yl)pyridin-5-yl)-3-fluorophenyl)-5-(hydroxymethyl)oxazolidin-2-one dihydrogen phosphate disodium salt
Torezolid phosphate disodium salt
CAS Number: 856867-39-5
Molecular Formula: C₁₇H₁₅FN₆O₆P • 2Na
Molecular Weight: 517.32 g/mol (anhydrous)
2. Structure & Properties
Appearance: White to off-white powder.
Solubility: Highly soluble in water (> 100 mg/mL), slightly soluble in ethanol, and practically insoluble in non-polar organic solvents. The disodium salt form significantly enhances aqueous solubility compared to the free acid or parent Tedizolid.
Role: Prodrug of the active antibacterial agent, Tedizolid (TR-700). Enzymatic hydrolysis (dephosphorylation) in vivo rapidly converts it to the active compound.
Chirality: Contains a single chiral center (oxazolidinone ring); the pharmacologically active enantiomer is specified.
3. Pharmacological Class & Mechanism of Action
Class: Second-generation oxazolidinone antibiotic.
Mechanism: The active metabolite, Tedizolid , inhibits bacterial protein synthesis by binding to the 23S ribosomal RNA of the 50S subunit. This prevents formation of the functional 70S initiation complex.
Target Pathogens: Primarily effective against Gram-positive bacteria, including multidrug-resistant strains:
Methicillin-resistant Staphylococcus aureus (MRSA)
Vancomycin-resistant Enterococcus faecium (VRE)
Penicillin-resistant Streptococcus pneumoniae (PRSP)
4. Key Applications
Active Pharmaceutical Ingredient (API): Used as the water-soluble salt form in the manufacture of sterile injectable formulations (IV) and potentially oral tablets/suspensions.
Therapeutic Indication: Treatment of acute bacterial skin and skin structure infections (ABSSSI) caused by susceptible Gram-positive organisms. Marketed under the brand name Sivextro (US)/ Sivextro (EU).
Research Tool: Used in microbiological, pharmacological, and pharmacokinetic studies investigating oxazolidinone antibiotics and resistance mechanisms.
5. Advantages over First-Gen Oxazolidinones (e.g., Linezolid)
Enhanced potency (4- to 16-fold greater in vitro activity against many Gram-positives).
Activity against some linezolid-resistant strains (e.g., those with certain cfr mutations or 23S rRNA mutations).
Once-daily dosing regimen.
Potentially reduced risk of myelosuppression (bone marrow suppression) with typical treatment durations.
6 . Handling & Storage
Storage: Store in a cool, dry place. Typically recommended at 2-8°C (refrigerated) or -20°C for long-term storage, protected from light and moisture. Desiccate.
Stability: Stable under recommended storage conditions. Protect from excessive heat and humidity. Solutions in water are typically stable for short periods under controlled conditions but should be used promptly according to formulation protocols.
Handling: Handle using standard laboratory safety precautions. Use personal protective equipment (PPE) including gloves and safety glasses. Avoid inhalation of dust and contact with skin/eyes.
