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Contezolid
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。
Contezolid图片
规格:98%
分子量:408.33
包装与价格:
包装价格(元)
5mg电议
10mg电议

产品介绍
Contezolid (MRX-I) 是一种新型的恶唑烷酮,用于耐药革兰氏阳性菌引起的皮肤组织感染并发症 (cSSTI) 的抗生素。Contezolid (MRX-I) 可显著降低骨髓移植和单胺氧化酶抑制。
货号:ajcx34254
CAS:1112968-42-9
分子式:C18H15F3N4O4
分子量:408.33
溶解度:DMSO : 120 mg/mL (293.88 mM; Need ultrasonic)
纯度:98%
存储:Store at -20°C
库存:现货

Background:

Contezolid (MRX-I), a new and oraly active oxazolidinone, is an antibiotic in study for complicated skin and soft tissue infections (cSSTI) caused by resistant Gram-positive bacteria. Contezolid (MRX-I) markedly reduces potential for myelosuppression and monoamine oxidase inhibition (MAOI)[1][2].

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].

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].

[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.