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Tedizolid Phosphate Sale

(Synonyms: 磷酸特地唑胺; TR-701FA) 目录号 : GC45006

A prodrug form of tedizolid

Tedizolid Phosphate Chemical Structure

Cas No.:856867-55-5

规格 价格 库存 购买数量
1mg
¥313.00
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5mg
¥702.00
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10mg
¥1,170.00
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25mg
¥4,699.00
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Sample solution is provided at 25 µL, 10mM.

Description

Tedizolid phosphate is a prodrug form of tedizolid, an antibiotic with activity against Gram-positive bacteria. Tedizolid phosphate is rapidly converted by non-specific phosphatases to tedizolid, which inhibits the growth of S. aureus, S. epidermidis, E. faecalis, E. faecium, S. pneumoniae, and S. pyogenes (MICs = 0.25-1 μg/ml). In vivo, tedizolid phosphate (15 mg/kg) reduces vegetation titer in a rabbit model of aortic valve endocarditis caused by methicillin-resistant S. aureus (MRSA). It also reduces densities of methicillin-susceptible S. aureus and MRSA infection in a mouse model of catheter-related biofilm infection and increases survival in a rabbit model of MRSA necrotizing pneumonia.

实验参考方法

Animal experiment:

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.

化学性质

Cas No. 856867-55-5 SDF
别名 磷酸特地唑胺; TR-701FA
Canonical SMILES FC1=C(C2=CN=C(C3=NN(C)N=N3)C=C2)C=CC(N4C(O[C@@H](COP(O)(O)=O)C4)=O)=C1
分子式 C17H16FN6O6P 分子量 450.3
溶解度 PBS (pH 7.2): 1 mg/ml 储存条件 Store at -20°C
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
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溶解性数据

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1 mg 5 mg 10 mg
1 mM 2.2207 mL 11.1037 mL 22.2074 mL
5 mM 0.4441 mL 2.2207 mL 4.4415 mL
10 mM 0.2221 mL 1.1104 mL 2.2207 mL
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