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(S)-Tedizolid
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
(S)-Tedizolid图片
CAS NO:1431699-67-0
规格:≥98%
包装与价格:
包装价格(元)
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW) 370.34
FormulaC17H15FN6O3
CAS No.1431699-67-0 ((S)-Tedizolid);
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: ≥ 10 mM
Water: ≥ 1 mg/mL
Ethanol: ≥ 1 mg/mL
Chemical Name(5S)-3-(3-fluoro-4-(6-(2-methyl-2H-tetrazol-5-yl)pyridin-3-yl)phenyl)-5-(hydroxymethyl)oxazolidin-2-one
Synonyms (S)-DA-7157; (S)-DA7157; DA 7157; (S)-TR-700; (S)-TR 700; TR700; (S)-Tedizolid; (S)-Torezolid.
实验参考方法
In Vitro

In vitro activity: Tedizolid (formerly known as torezolid, TR-700, or DA-7157, trade name Sivextro), is an oxazolidinone-class antibiotic against Gram-positive bacteria. The mechanism of action is to inhibit protein synthesis by binding to the 50S ribosomal subunit of the G+ bacteria. Tedizolid phosphate is a phosphate ester prodrug of the active compound tedizolid. It was developed by Cubist Pharmaceuticals, following acquisition of Trius Therapeutics (formerly Dong-A Pharmaceuticals in Korea), and is approved in 2014 by the US-FDA for the treatment of acute bacterial skin and skin structure infections (also known as complicated skin and skin-structure infections (cSSSIs)).


Kinase Assay: Tedizolid (0.25 μg/mL) inhibits all 28 clinical isolates of PRSP, and is 4-fold more potent than linezolid against PRSP


Cell Assay: Tedizolid (0.25 μg/mL) inhibits all 28 clinical isolates of PRSP, and is 4-fold more potent than linezolid against PRSP

In Vivo 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, to induce a systemic S. pneumoniae infection. 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.
Animal model 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, to induce a systemic S. pneumoniae infection.
Formulation & Dosage 40 mg/kg of body weight, 13.33 mg/kg, 4.44 mg/kg, and 1.48 mg/kg; i.p.
References Antimicrob Agents Chemother. 2012 Sep;56(9):4713-7.