Contezolid|1112968-42-9|(MRX-I)-陌孚医药/Medlife

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Contezolid (Synonyms: MRX-I)

目录号: PL07509 纯度: ≥99%

CAS No. :1112968-42-9

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中文名称	Contezolid
英文名称	Contezolid
英文别名	MRX-I;Contezolid;MRX-1;B669M62ELP;(5S)-5-[(1,2-oxazol-3-ylamino)methyl]-3-[2,3,5-trifluoro-4-(4-oxo-2,3-dihydropyridin-1-yl)phenyl]-1,3-oxazolidin-2-one;Contezolid [USAN];Contezolid (USAN/INN);GTPL10795;BDBM50017203;DB12796;SB17481;D11297;Q27274420;(S)-5-((isoxazol-3-ylamino)methyl)-3-(2,3,5-trifluoro-4-(4-oxo-3,4-dihydropyridin-1(2H)-yl)phenyl)oxazolidin-2-one;1-{2,3,6-trifluoro-4-[(5S)-5-{[(1,2-oxazol-3-yl)amino]methyl}-2-oxo-1,3-oxazol;contézolid;contezolidum
Cas No.	1112968-42-9
分子式	C₁₈H₁₅F₃N₄O₄
分子量	408.33
包装储存	4°C, sealed storage, away from moisture and light In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

产品详情

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。

生物活性

Contezolid (MRX-I), a new and orally 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).

性状

Solid

IC50 & Target[1][2]

Oxazolidinone

体外研究(In Vitro)

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

体内研究(In Vivo)

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 C max /dose was 524, 1065, and 259 ng/mL/(mg/kg); dose-normalized AUC 0?t /dose was 1654, 3703, and 1664 ng?h/mL/(mg/kg); T 1/2 is 1, 1.5, and 3 h; and the oral bioavailability is 69%, 109%, and 37%.
Contezolid (MRX-I) exhibits no obvious toxicity.
Contezolid (MRX-I, 100 mg/kg, once daily) significantly reduced the bacterial load in lungs compared to the untreated early and late controls.
has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture and light In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

ClinicalTrial

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.

溶解度数据	In Vitro: DMSO : 120 mg/mL (293.88 mM; Need ultrasonic)配制储备液

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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