化學(xué)名

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

簡稱

Tedizolid

別名

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

中文名

特地唑胺

化學(xué)式

C₁₇H₁₅FN₆O₃

分子量

370.34

CAS號

856866-72-3

純度

98%

溶劑/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。

產(chǎn)品描述

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

信號通路

Anti-infection

靶點

MAO-A

MAO-B

－

－

－

IC50

8.7μM

5.7μM

－

－

－

體外研究

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.

體內(nèi)研究

N/A

臨床實驗

N/A

特征

N/A

酶活性檢測實驗

方法

N/A

細(xì)胞實驗

細(xì)胞系

N/A

濃度

N/A

處理時間

N/A

方法

N/A

動物實驗

動物模型

N/A

配制

N/A

劑量

N/A

給藥方式

N/A

產(chǎn)品編號

產(chǎn)品名稱

包裝

SC3265-10mM

Tedizolid (MAO-A抑制劑)

10mM×0.2ml

SC3265-5mg

Tedizolid (MAO-A抑制劑)

5mg

SC3265-25mg

Tedizolid (MAO-A抑制劑)

25mg

—

說明書

1份