|N-(5-氨基吡啶-2-基)-4-(三氟甲基)苯甲酰胺|CsnPharm

CAS No.: 1011244-68-0

TFAP Catalog No. CSN22602

Synonyms: N-(5-Aminopyridin-2-yl)-4-(trifluoromethyl)benzamide;COX-1 Inhibitor IV

TFAP is a cell-permeable pyridinyl-benzamide compound that acts as a COX-1-selective inhibitor (IC50 = 0.80 and 210 µM against ovine COX-1 and COX-2, respectively).

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述Biosynthesis of prostaglandins from arachidonic acid (AA) is catalyzed by cyclooxygenase (COX), which exists as COX-1 and COX-2. AA is in turn released from the cell membrane upon neopathological stimuli. COX inhibitors interfere in this catalytic and disease onset process^[1]. TFAP is a selective COX-1 inhibitor with an IC₅₀ value of 0.8 μM. Although TFAP shows potent analgesic effect without gastric damage, the urine after administration of TFAP becomes red-purple^[2].
临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT02238015	-	-	Unknown	March 2015	China, Zhejiang ... more >> Wenzhou Medical University Recruiting WenZhou, Zhejiang, China, 325027 Contact: Qian Zheng, MD 18367839685 zq15.04@163.com Collapse <<

参考文献

[1] Vitale P, Panella A, Scilimati A, Perrone MG. COX-1 Inhibitors: Beyond Structure Toward Therapy. Med Res Rev. 2016;36(4):641‐671
[2] Kakuta H, Fukai R, Xiaoxia Z, et al. Identification of urine metabolites of TFAP, a cyclooxygenase-1 inhibitor. Bioorg Med Chem Lett. 2010;20(6):1840‐1843

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.5558 mL
- 17.7788 mL
- 35.5577 mL
- 5 mM
- 0.7112 mL
- 3.5558 mL
- 7.1115 mL
- 10 mM
- 0.3556 mL
- 1.7779 mL
- 3.5558 mL

技术信息

CAS号

1011244-68-0

储存条件

粉末: Keep in dark place,Inert atmosphere,Room temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C13H10F3N3O

运输

蓝冰

分子量

281.23

别名

N-(5-Aminopyridin-2-yl)-4-(trifluoromethyl)benzamide;COX-1 Inhibitor IV

溶解度

DMSO	200.0 mg/mL (711.2 mM)
Water	insoluble

动物实验配方

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TFAP Catalog No. CSN22602

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