Tedizolid 纯度:98.69% 5mg

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Tedizolid 纯度:98.69% 5mg

市场价：: 1200.00

促销价：: ¥1200.00

货号：HY-14855

品牌：MCE

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北京朝阳

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商品介绍
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Tedizolid是一种新型恶唑烷酮，通过与核糖体50S亚基的23S核糖体RNA结合来抑制细菌 (bacterial) 的蛋白质合成。

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.

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].

Solvent & Solubility

In Vitro:

10 mM in DMSO

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.7002 mL	13.5011 mL	27.0022 mL
5 mM	0.5400 mL	2.7002 mL	5.4004 mL
10 mM	0.2700 mL	1.3501 mL	2.7002 mL

* Please refer to the solubility information to select the appropriate solvent.

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.

Animal Administration ^[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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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.

Animal Administration
^[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.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References