您好,欢迎来到化工原料网! [登录] [免费注册]
化工原料网
位置:首页 > 产品库 > Tedizolid HCl
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
Tedizolid HCl
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。
Tedizolid HCl图片
包装与价格:
包装价格(元)
5mg电议
10mg电议
50mg电议

产品介绍

Oxazolidinone for gram-positive infections

化学名(R)-3-(3-fluoro-4-(6-(2-methyl-2H-tetrazol-5-yl)pyridin-3-yl)phenyl)-5-(hydroxymethyl)oxazolidin-2-one hydrochloride
Canonical SMILESFC1=CC(N2C[C@H](CO)OC2=O)=CC=C1C3=CC=C(C4=NN(C)N=N4)N=C3.Cl
分子式C17H16ClFN6O3
分子量406.80
溶解度≥ 13.57mg/mL in DMSO with gentle warming, Limited solubility in EtOH
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

IC50: for MAO-A (monoamine oxidase-A), 8.7 uM; for MAO-B, 5.7 uM.
Tedizolid HCl is a reversible, novel oxazolidinone antibiotic. It is the first oxazolidinone to be approved since linezolid in 2000. Tedizolid phosphate is the second commercially available oxazolidinone antibiotic and is the prodrug form of tedizolid with a fixed once-daily dose. As an expanded-spectrum oxazolidinone it has potent activity against a wide range of Gram-positive pathogens [1].
In vitro: In vitro, tedizolid was a reversible inhibitor for both human MAO-A and MAO-B; for MAO-A, the value of IC50 was 8.7 uM, and for MAO-B, the value of IC50 was 5.7 uM. For this two inhibitions, add 46.0 and 2.1 uM of linezolid, respectively would be better [2].
In vivo: It exhibited not only a potent activity against Gram-positive pathogens but also maintained activity against linezolid resistant bacteria. In murine serotonergic model, the number of head twitches was analyzed after tedizolid phosphate was administrated by intraperitoneal injection [2].
Clinical trial: With 200 mg once daily tedizolid would treat the acute bacterial skin and skin structure infections caused by gram-positive bacteria in phase III clinical trials. The treatment effects of tedizolid for ventilator-acquired and health care-associated pneumonia were currently investigated [3].
References:
[1] Chen KH, Huang YT, Liao CH et dl. In Vitro Activities of Tedizolid and Linezolid against Gram-Positive Cocci Associated with Acute Bacterial Skin and Skin Structure Infections and Pneumonia. Antimicrob Agents Chemother. 2015 Oct;59(10):6262-5.
[2] S. Flanagan, K. Bartizal, S. L. Minassian et dl. In Vitro, In Vivo, and Clinical Studies of Tedizolid To Assess the Potential for Peripheral or Central Monoamine Oxidase Interactions. Antimicrob Agents Chemother. 2013 Jul;57(7):3060-6.
[3] Rybak JM, Marx K, Martin CA. Early experience with tedizolid: clinical efficacy, pharmacodynamics, and resistance. Pharmacotherapy. 2014 Nov;34(11):1198-208.