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  3. Tolfenamic Acid

Tolfenamic Acid  (Synonyms: 托芬那酸; GEA 6414)

目录号: HY-B0335 纯度: 99.94%
COA 产品使用指南

Tolfenamic Acid (GEA 6414) 是一种非甾体抗炎剂和抗癌剂,能够选择性地抑制 COX-2 的活性,在 LPS 诱导的犬 DH82 单核细胞/巨噬细胞中,对 COX-2IC50 值为 13.49 μM (3.53 μg/mL),对 COX-1 无作用。

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Tolfenamic Acid Chemical Structure

Tolfenamic Acid Chemical Structure

CAS No. : 13710-19-5

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规格 价格 是否有货 数量
Free Sample (0.1 - 0.2 mg)   Apply now  
10 mM * 1 mL in DMSO ¥500
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500 mg ¥400
In-stock
1 g ¥500
In-stock
10 g ¥1500
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50 g   询价  

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Other Forms of Tolfenamic Acid:

MCE 顾客使用本产品发表的 1 篇科研文献

查看 COX 亚型特异性产品:

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

Tolfenamic Acid (GEA 6414) is a non-steroidal anti-inflammatory and anti-cancer agent, selectively inhibits COX-2, with an IC50 of 13.49 μM (3.53 μg/mL) in LPS-treated (COX-2) canine DH82 monocyte/macrophage cells, but shows no effect on COX-1.

IC50 & Target[1]

COX-2

13.49 μM (IC50, in cell)

体外研究
(In Vitro)

Tolfenamic Acid (GEA 6414) 是一种非甾体抗炎剂,选择性抑制 COX-2,在 LPS 处理的 (COX-2) 犬 DH82 单核细胞中的 IC50 为 13.49 μM (3.53 μg/mL)/巨噬细胞,但对 COX-1 没有影响[1]
Tolfenamic Acid (GEA 6414) (100 μM) 抑制 BE3、OE33 和 SKGT5 的 >70% 的细胞活力。Tolfenamic Acid (GEA 6414) 也是一种有效的 Sp 蛋白抑制剂,可降低 Sp1 和 Sp4,并抑制食管癌细胞 BE3 和 SKGT5 中的 c-Met 表达[2]
Tolfenamic Acid (GEA 6414) (50 μM) 显著影响 L3.6pl 细胞中的基因表达,并下调 CENPF、KIF20A、LMNB1、MYB、SKP2、CCNE2 和 DDIT3[3]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Tolfenamic Acid (GEA 6414) (50 mg/kg 3 次/周,口服) 抑制 N-亚硝基甲基苄胺 (NMBA) 诱导的食管肿瘤模型中的肿瘤形成和肿瘤发病率。Tolfenamic Acid (GEA 6414) 还会导致接受 NMBA 处理的大鼠的肿瘤多样性和肿瘤体积减少[2]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
分子量

261.70

Formula

C14H12ClNO2

CAS 号
性状

固体

颜色

White to off-white

中文名称

托芬那酸;托灭酸

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性数据
In Vitro: 

DMSO 中的溶解度 : ≥ 100 mg/mL (382.12 mM; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

H2O 中的溶解度 : < 0.1 mg/mL (insoluble)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.8212 mL 19.1058 mL 38.2117 mL
5 mM 0.7642 mL 3.8212 mL 7.6423 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

In Vivo:

请根据您的 实验动物和给药方式 选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 方案 一

    请依序添加每种溶剂: 10% DMSO    90% Corn Oil

    Solubility: ≥ 2.08 mg/mL (7.95 mM); 澄清溶液

    此方案可获得 ≥ 2.08 mg/mL(饱和度未知)的澄清溶液,此方案实验周期在半个月以上的动物实验酌情使用。

    1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
请输入您的动物体内配方组成:
%
DMSO +
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。
您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
连续给药周期超过半月以上,请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
纯度 & 产品资料

纯度: 99.94%

参考文献
Cell Assay
[2]

All cells are grown in media (RPMI1640) supplemented with 5% serum and cultured at 37°C in a humidified atmosphere of 95% air and 5% CO2. Twenty four hours after seeding, cells are treated with vehicle (0.1% DMSO) or various concentrations of Tolfenamic Acid (GEA 6414) (25/50/100 μM). Cell viability assays are conducted at 24, 48 and 72 h post-treatment. Cells are treated with 50 μM Tolfenamic Acid (GEA 6414) and the cell pellets are harvested at 48 h post-treatment. These pellets are used to prepare cell lysates that are used in Western blot analyses[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[2]

Mice[2]
The Fischer 344 (F-344) rat model of esophageal SCC are initially housed two per cage, but eventually separated to one per cage due to increase in size, and are maintained under standard, humane conditions (20±2°C, 50±10% relative humidity, 12-h light/dark cycles). Food and water are provided ad libitum. Body weights are recorded at the time of each dosing. Two weeks after arrival in the animal facility, the rats are randomLy assigned into 4 groups: C: NMBA (1-5 week); NTA: (NMBA 1-5 week and then Tolfenamic Acid (GEA 6414) 6-25 week); NC: Negative control (vehicle); and TA: Tolfenamic Acid (GEA 6414) negative control. Control (C) and NTA groups are injected s.c. with NMBA (0.5 mg/kg) in 0.2 mL vehicle three times per week for 5 weeks while negative control groups are injected with vehicle alone. NTA and Tolfenamic Acid groups also receive 50 mg/kg Tolfenamic Acid (GEA 6414) by oral gavage from week 6 through week 25. After the 25th week, the animals are sacrificed, esophagi are cut open longitudinally, and surface tumors are mapped and counted. The number and the size of lesions, including polyps are recorded and images captured. Tumor volume is calculated using the formula for a prolate spheroid: length × width × height × p/6[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献

Tolfenamic Acid 相关分类

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.8212 mL 19.1058 mL 38.2117 mL 95.5292 mL
5 mM 0.7642 mL 3.8212 mL 7.6423 mL 19.1058 mL
10 mM 0.3821 mL 1.9106 mL 3.8212 mL 9.5529 mL
15 mM 0.2547 mL 1.2737 mL 2.5474 mL 6.3686 mL
20 mM 0.1911 mL 0.9553 mL 1.9106 mL 4.7765 mL
25 mM 0.1528 mL 0.7642 mL 1.5285 mL 3.8212 mL
30 mM 0.1274 mL 0.6369 mL 1.2737 mL 3.1843 mL
40 mM 0.0955 mL 0.4776 mL 0.9553 mL 2.3882 mL
50 mM 0.0764 mL 0.3821 mL 0.7642 mL 1.9106 mL
60 mM 0.0637 mL 0.3184 mL 0.6369 mL 1.5922 mL
80 mM 0.0478 mL 0.2388 mL 0.4776 mL 1.1941 mL
100 mM 0.0382 mL 0.1911 mL 0.3821 mL 0.9553 mL
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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