Tedizolid phosphateTedizolid phosphate
MedChemExpress (MCE)
HY-14855B
856867-55-5
TR-701FA
99.65%
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Room temperature in continental US
may vary elsewhere.
Tedizolid phosphate (TR-701FA) is a MAO-A and MAO-B inhibitor with activity against Gram-positive bacteria.
Tedizolid phosphate (TR-701FA
0.25 μg/mL) inhibits all 28 clinical isolates of PRSP, and is 4-fold more potent than linezolid against PRSP[1].
For mice infected with PSSP type III, the 100% survival rate is achieved with tedizolid phosphate (TR-701FA) at a minimum total daily dose of 10 mg/kg. Lungs of infected mice treated with tedizolid phosphate show less severe inflammation and edema, as indicated by the mean scores for inflammation and edema[1].
To induce a systemic S. pneumoniae infection, male ICR mice (weight, 18 to 20 g) are inoculated intraperitoneally with 1 of 4 PRSP isolates (DR9, DR10, DR11, or DR14) suspended in 10% mucin. The suspension contained sufficient bacteria to kill 100% of untreated control mice. At 1 h postinfection, mice receives a single dose of either tedizolid phosphate or linezolid, and survival is assessed daily for 7 days postinfection. Treatments are delivered both orally and intravenously at each of four doses (40 mg/kg of body weight, 13.33 mg/kg, 4.44 mg/kg, and 1.48 mg/kg), with 8 mice per group defined by dose, delivery method, and infecting strain. The 50% effective dose (ED50), i.e., the dose allowing survival of 50% of the infected mice, is calculated for each delivery route using probit analysis.
MAO-A MAO-B
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[1]. Choi S, et al. Activity of Tedizolid Phosphate (TR-701) in Murine Models of Infection with Penicillin-resistant and Penicillin-sensitive Streptococcus pneumoniae. Antimicrob Agents Chemother. 2012 Jun 19. [Content Brief]