CAS 856866-72-3|Tedizolid

Introduction:Basic information about CAS 856866-72-3|Tedizolid, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
Common NameTedizolid
CAS Number856866-72-3Molecular Weight370.338
Density1.6±0.1 g/cm3Boiling Point614.5±65.0 °C at 760 mmHg
Molecular FormulaC17H15FN6O3Melting Point/
MSDS/Flash Point325.4±34.3 °C

Names

Nametedizolid
SynonymMore Synonyms

Tedizolid BiologicalActivity

DescriptionTedizolid is a novel oxazolidinone, acting through inhibition of bacterial protein synthesis by binding to 23S ribosomal RNA (rRNA) of the 50S subunit of the ribosome.
Related CatalogSignaling Pathways >>Anti-infection >>BacterialResearch Areas >>Infection
In VitroTedizolid (0.25 μg/mL) inhibits all 28 clinical isolates of PRSP, and is 4-fold more potent than linezolid against PRSP[1].
In VivoFor mice infected with PSSP type III, the 100% survival rate is achieved with tedizolid phosphate 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].
Animal AdminTo 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.
References

[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.

Chemical & Physical Properties

Density1.6±0.1 g/cm3
Boiling Point614.5±65.0 °C at 760 mmHg
Molecular FormulaC17H15FN6O3
Molecular Weight370.338
Flash Point325.4±34.3 °C
Exact Mass370.118958
PSA106.26000
LogP1.56
Vapour Pressure0.0±1.9 mmHg at 25°C
Index of Refraction1.725
InChIKeyXFALPSLJIHVRKE-GFCCVEGCSA-N
SMILESCn1nnc(-c2ccc(-c3ccc(N4CC(CO)OC4=O)cc3F)cn2)n1

Safety Information

HS Code29339900

Synonyms

(5R)-3-{3-Fluoro-4-[6-(2-methyl-2H-tetrazol-5-yl)-3-pyridinyl]phenyl}-5-(hydroxymethyl)-1,3-oxazolidin-2-one
Torezolid
TR-701
(5R)-3-[3-fluoro-4-[6-(2-methyltetrazol-5-yl)pyridin-3-yl]phenyl]-5-(hydroxymethyl)-1,3-oxazolidin-2-one
TR-700
(R)-3-(4-(2-(2-methyltetrazol-5-yl)pyridin-5-yl)-3-fluorophenyl)-5-hydroxymethyl oxazolidin-2-one
Tedizolid [USAN:INN]
2-Oxazolidinone, 3-[3-fluoro-4-[6-(2-methyl-2H-tetrazol-5-yl)-3-pyridinyl]phenyl]-5-(hydroxymethyl)-, (5R)-
UNII:97HLQ82NGL
Tedizolid
(5R)-3-{3-fluoro-4-[6-(2-methyl-2H-tetrazol-5-yl)pyridin-3-yl]phenyl}-5-(hydroxymethyl)-2-oxazolidinone
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