Tedizolid (MAO-A抑制剂)

化学名

3-[3-fluoro-4-[6-(2-methyltetrazol-5-yl)pyridin-3-yl]phenyl]-5-(hydroxymethyl)-1,3-oxazolidin-2-one

简称

Tedizolid

别名

TR-700, DA-7157, Torezolid, TR 700, DA 7157

中文名

特地唑胺

化学式

C₁₇H₁₅FN₆O₃

分子量

370.34

CAS号

856866-72-3

纯度

98%

溶剂/溶解度

Water<1mg/ml; DMSO4mg/ml; Ethanol<1mg/ml

溶液配制

5mg加入1.35ml DMSO，或者每3.7mg加入1ml DMSO，配制成10mM溶液。SC3265-10mM用DMSO配制。

产品描述

Torezolid (TR-701; tedizolid) is a novel oxazolidinone for gram-positive infections.

信号通路

Anti-infection

靶点

MAO-A

MAO-B

－

－

－

IC50

8.7μM

5.7μM

－

－

－

体外研究

Tedizolid was reversible inhibitors of human MAO-A and MAO-B; the 50% inhibitory concentration (IC50) for tedizolid was 8.7μM for MAO-A and 5.7μM for MAO-B. Tedizolid phosphate was negative in the mouse head twitch model of serotonergic activity. Two randomized placebo-controlled crossover clinical studies assessed the potential of 200mg/day tedizolid phosphate (at steady state) to enhance pressor responses to coadministered oral tyramine or pseudoephedrine. Sensitivity to tyramine was determined by comparing the concentration of tyramine required to elicit a ≥30mmHg increase in systolic blood pressure (TYR30) when administered with placebo versus tedizolid phosphate. The geometric mean tyramine sensitivity ratio (placebo TYR30/tedizolid phosphate TYR30) was 1.33; a ratio of ≥2 is considered clinically relevant. In the pseudoephedrine study, mean maximum systolic blood pressure was not significantly different when pseudoephedrine was coadministered with tedizolid phosphate versus placebo.

体内研究

N/A

临床实验

N/A

特征

N/A

酶活性检测实验

方法

N/A

细胞实验

细胞系

N/A

浓度

N/A

处理时间

N/A

方法

N/A

动物实验

动物模型

N/A

配制

N/A

剂量

N/A

给药方式

N/A

产品编号

产品名称

包装

SC3265-10mM

Tedizolid (MAO-A抑制剂)

10mM×0.2ml

SC3265-5mg

Tedizolid (MAO-A抑制剂)

5mg

SC3265-25mg

Tedizolid (MAO-A抑制剂)

25mg

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说明书

1份