Radezolid

Radezolid is an oxazolidinone antibiotic and a derivative of linezolid (Cay-15012). It is active against a variety of bacterial clinical isolates, including strains of methicillin-sensitive and -resistant S. aureus, vancomycin-sensitive and -resistant E. faecalis and E. faecium, and linezolid-resistant S. aureus, S. epidermidis, E. faecalis, E. faecium, and S. pneumoniae (MICs = =0.25-64 µg/ml). Radezolid is also active against L. monocytogenes, S. aureus, L. pneumophila, and S. epidermidis in THP-1 macrophages (EC50s = 0.62, 0.63, 8.45, and 2.99 mg/L, respectively). It inhibits protein translation in isolated wild-type and linezolid-resistant S. aureus 70S ribosomes but not rabbit reticulocyte lysates (IC50s = 0.02, 0.03, and >2 µM, respectively). Radezolid is efficacious in a mouse model of S. pneumoniae-induced peritonitis with a 50% protective dose (PD50) value of 1.3 mg/kg per day.Formal Name: N-[[(5S)-3-[2-fluoro-4'-[[(1H-1,2,3-triazol-5-ylmethyl)amino]methyl][1,1'-biphenyl]-4-yl]-2-oxo-5-oxazolidinyl]methyl]-acetamide. CAS Number: 869884-78-6. Synonyms: Rx-01_667, RX-1741. Molecular Formula: C22H23FN6O3. Formula Weight: 438.5. Purity: >95%. Formulation: (Request formulation change), A solid. Solubility: DMF: 2mg/mL, DMSO: 2mg/mL, DMSO:PBS (pH 7.2) (1:3): 0.25mg/mL. SMILES: O=C1N(C2=CC=C(C3=CC=C(CNCC4=CN=NN4)C=C3)C(F)=C2)C[C@H](CNC(C)=O)O1. InChi Code: InChI=1S/C22H23FN6O3/c1-14(30)25-12-19-13-29(22(31)32-19)18-6-7-20(21(23)8-18)16-4-2-15(3-5-16)9-24-10-17-11-26-28-27-17/h2-8,11,19,24H,9-10,12-13H2,1H3,(H,25,30)(H,26,27,28)/t19-/m0/s1. InChi Key: BTTNOGHPGJANSW-IBGZPJMESA-N.