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Thiophene-2

Thiophene-2用途

Thiophene-2 (TP2) 是一种特定的 Pks13 抑制剂。Thiophene-2 抑制分枝酸的生物合成,并迅速导致分枝杆菌细胞死亡。Thiophene-2 对结核分枝杆菌具有活性,MIC 值为 1 μM,并具有有效的抗结核活性。
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Thiophene-2名称

[ CAS 号 ]:
420089-51-6

[ 英文名 ]:
TP2

[英文别名 ]:

Thiophene-2生物活性

[ 描述 ]:

Thiophene-2 (TP2) 是一种特定的 Pks13 抑制剂。Thiophene-2 抑制分枝酸的生物合成,并迅速导致分枝杆菌细胞死亡。Thiophene-2 对结核分枝杆菌具有活性,MIC 值为 1 μM,并具有有效的抗结核活性。

[ 相关类别 ]:

研究领域 >> 感染
信号通路 >> 抗感染 >> 细菌

[ 靶点 ]

MIC: 1 μM (Mycobacterium tuberculosis)


[体外研究]

体外脂肪负荷,抑制脂肪酸激酶3。噻吩-2(TP2;0-125μM)以剂量依赖的方式抑制野生型结核分枝杆菌(Mtb)Pks13(Pks13_-WT)的负载。噻吩-2还抑制棕榈酸(FL C16)负载到抗TP的F79S突变蛋白上[1]。噻吩-2对猴肾Vero细胞和人肝癌HepG2细胞的IC50分别为17.5和7.30μM。当噻吩-2浓度为12.8μM时,在卡介苗感染的J774A.1巨噬细胞内观察到显著的细胞内杀伤活性[1]。

[参考文献]

[1]. Regina Wilson, et al. Antituberculosis Thiophenes Define a Requirement for Pks13 in Mycolic Acid Biosynthesis. Nat Chem Biol. 2013 Aug;9(8):499-506.

Thiophene-2物理化学性质

[ 分子式 ]:
C18H14F5NO3S

[ 分子量 ]:
419.37

[ 储存条件 ]:
2-8°C,避光,干燥,密封

Thiophene-2安全信息

[ 危害码 (欧洲) ]:
Xi

[ 危险品运输编码 ]:
NONH for all modes of transport

Thiophene-2文献

Greater Sensitivity of Blood Pressure Than Renal Toxicity to Tyrosine Kinase Receptor Inhibition With Sunitinib.

Hypertension 66 , 543-9, (2015)

Hypertension and renal injury are off-target effects of sunitinib, a tyrosine kinase receptor inhibitor used for the treatment of various tumor types. Importantly, these untoward effects are accompani...

A method to quantitate the neutralizing capacity of anti-therapeutic protein antibodies in serum and their correlation to clinical impact.

J. Pharm. Biomed. Anal. 102 , 176-83, (2014)

A robust, quantitative method for assessing the neutralizing capacity of anti-therapeutic protein antibodies was developed and tested using 4 analytical assay platforms typically used for detection of...

Effect of a grain challenge on ruminal, urine, and fecal pH, apparent total-tract starch digestibility, and milk composition of Holstein and Jersey cows.

J. Dairy Sci. 99 , 2190-200, (2016)

The effects of a grain challenge on ruminal, urine, and fecal pH, apparent total-tract starch digestibility, and milk composition were determined. Six Holstein cows, 6 rumen-cannulated Holstein cows, ...


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公司名:上海化源生化科技有限公司

区域:上海市普陀区

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联系人:徐经理

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