Tedizolid

Modify Date: 2024-01-02 18:45:30

Tedizolid Structure
Tedizolid structure
Common Name Tedizolid
CAS Number 856866-72-3 Molecular Weight 370.338
Density 1.6±0.1 g/cm3 Boiling Point 614.5±65.0 °C at 760 mmHg
Molecular Formula C17H15FN6O3 Melting Point N/A
MSDS N/A Flash Point 325.4±34.3 °C

 Use of Tedizolid


Tedizolid 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.

 Names

Name tedizolid
Synonym More Synonyms

 Tedizolid Biological Activity

Description Tedizolid 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 Catalog
In Vitro Tedizolid (0.25 μg/mL) inhibits all 28 clinical isolates of PRSP, and is 4-fold more potent than linezolid against PRSP[1].
In Vivo For 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 Admin 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.
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

Density 1.6±0.1 g/cm3
Boiling Point 614.5±65.0 °C at 760 mmHg
Molecular Formula C17H15FN6O3
Molecular Weight 370.338
Flash Point 325.4±34.3 °C
Exact Mass 370.118958
PSA 106.26000
LogP 1.56
Vapour Pressure 0.0±1.9 mmHg at 25°C
Index of Refraction 1.725

 Safety Information

HS Code 29339900

 Synthetic Route

~84%

Tedizolid Structure

Tedizolid

CAS#:856866-72-3

Literature: TRIUS THERAPEUTICS; COSTELLO, Carrie, A.; SIMSON, Jaqueline, A.; DUGUID, Robert, J.; PHILLIPSON, Douglas Patent: WO2010/42887 A2, 2010 ; Location in patent: Page/Page column 19-20 ;

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Tedizolid Structure

Tedizolid

CAS#:856866-72-3

Literature: European Journal of Medicinal Chemistry, , vol. 46, # 4 p. 1027 - 1039

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Tedizolid Structure

Tedizolid

CAS#:856866-72-3

Literature: European Journal of Medicinal Chemistry, , vol. 46, # 4 p. 1027 - 1039

 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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Price: $132/10mM*1mLinDMSO

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