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Contezolid acefosamil sodium

产品编号 T36441 CAS 1807365-35-0

Contezolid acefosamil sodium (MRX-4) is a novel orally active oxazolidinone antibiotic under investigation for the treatment of complicated skin and soft tissue infections (cSSTI) caused by drug-resistant Gram-positive bacteria. It possesses strong efficacy against these pathogens while significantly minimizing the risks of myelosuppression and monoamine oxidase inhibition (MAOI) [1][2].

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Contezolid acefosamil sodium Chemical Structure

Contezolid acefosamil sodium, CAS 1807365-35-0

规格	价格/CNY		货期	数量
5 mg	￥ 7,419		待询
10 mg	￥ 11,712		待询

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其他形式的 Contezolid acefosamil sodium:

Contezolid acefosamil
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生物活性

化学信息

存储 & 溶解度

参考文献

产品描述	Contezolid acefosamil sodium (MRX-4) is a novel orally active oxazolidinone antibiotic under investigation for the treatment of complicated skin and soft tissue infections (cSSTI) caused by drug-resistant Gram-positive bacteria. It possesses strong efficacy against these pathogens while significantly minimizing the risks of myelosuppression and monoamine oxidase inhibition (MAOI) [1][2].
体外活性	Contezolid (MRX-I) is highly potent against all Grampositive clinical isolates of staphylococci, streptococci, and enterococci, including MDR organisms such as MRSA, methicilline-resistant Streptococcus epidermidis (MRSE), penicillin-resistant Streptococci (PRSP), and VRE[2].
体内活性	Oral absorption of Contezolid (MRX-I) occurrs rapidly in mouse, rat, and dog, with peak plasma concentrations observed at 0.5-2.6 h postdose. In mouse, rat, and dog, respectively, PK parameters are determined as follows: dose-normalized Cmax/dose was 524, 1065, and 259 ng/mL/(mg/kg); dose-normalized AUC0-t/dose was 1654, 3703, and 1664 ng?h/mL/(mg/kg); T1/2 is 1, 1.5, and 3 h; and the oral bioavailability is 69%, 109%, and 37%[2].Contezolid (MRX-I) exhibits no obvious toxicity[2].Contezolid (MRX-I, 100 mg/kg, once daily) significantly reduced the bacterial load in lungs compared to the untreated early and late controls[3].

分子量	553.343
分子式	C20H18F3N4NaO8P
CAS No.	1807365-35-0

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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参考文献

1. Junzhen Wu, et al. Evaluation of the Effect of Contezolid (MRX-I) on the Corrected QT Interval in a Randomized, Double-Blind, Placebo- and Positive-Controlled Crossover Study in Healthy Chinese Volunteers. Antimicrob Agents Chemother. 2020 May 21;64(6):e02158-19. 2. Mikhail F Gordeev, et al. New potent antibacterial oxazolidinone (MRX-I) with an improved class safety profile. J Med Chem. 2014 Jun 12;57(11):4487-97. 3. Carolyn Shoen, et al. In Vitro and In Vivo Activities of Contezolid (MRX-I) against Mycobacterium tuberculosis. Antimicrob Agents Chemother. 2018 Jul 27;62(8):e00493-18.

剂量换算

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体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

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第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

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