化学信息:
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
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化学式
|
C17H15FN6O3
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分子量
|
370.34
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CAS号
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856866-72-3
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纯度
|
98%
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溶剂/溶解度
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Water<1mg/ml; DMSO4mg/ml; Ethanol<1mg/ml
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溶液配制
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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。
|
生物信息:
产品描述
|
Torezolid (TR-701; tedizolid) is a novel oxazolidinone for gram-positive infections.
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信号通路
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Anti-infection
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靶点
|
MAO-A
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MAO-B
|
-
|
-
|
-
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IC50
|
8.7μM
|
5.7μM
|
-
|
-
|
-
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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
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临床实验
|
N/A
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特征
|
N/A
|
相关实验数据(此数据来自于公开文献,碧云天并不保证其有效性):
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
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给药方式
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N/A
|
参考文献:
1. Keel RA, Tessier PR, Crandon JL, Nicolau DP. Antimicrob Agents Chemother. 2012 Aug, 56(8), 4403-7.
2. Sahre M, Sabarinath S, Grant M, Seubert C, Deanda C, Prokocimer P, Derendorf H. Int J Antimicrob Agents. 2012 Jul, 40(1), 51-4.
3. Kanafani ZA, Corey GR. Expert Opin Investig Drugs. 2012 Apr, 21(4), 515-22.
包装清单:
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
|
—
|
说明书
|
1份
|
保存条件:
-20℃保存,至少一年有效。5mg和25mg包装也可室温保存,至少6个月有效。如果溶于非DMSO溶剂,建议分装后-80℃保存,预计6个月内有效。
注意事项:
本产品对人体有刺激性,操作时请小心,并注意适当防护以避免直接接触人体或吸入体内。
本产品仅限于专业人员的科学研究用,不得用于临床诊断或治疗,不得用于食品或药品,不得存放于普通住宅内。
为了您的安全和健康,请穿实验服并戴一次性手套操作。