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Tolfenamic Acid/托灭酸 {[allProObj[0].p_purity_real_show]}

货号:A127860 同义名: 托芬那酸 / GEA 6414; Clotam

Tolfenamic Acid是一种选择性 COX2 抑制剂,IC50 为 13.49 μM,是一种非甾体抗炎药(NSAID)。

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Tolfenamic Acid/托灭酸 化学结构 CAS号:13710-19-5
Tolfenamic Acid/托灭酸 化学结构
CAS号:13710-19-5
Tolfenamic Acid/托灭酸 3D分子结构
CAS号:13710-19-5
Tolfenamic Acid/托灭酸 化学结构 CAS号:13710-19-5
Tolfenamic Acid/托灭酸 3D分子结构 CAS号:13710-19-5
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Tolfenamic Acid/托灭酸 纯度/质量文件 产品仅供科研

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产品名称 COX COX-1 COX-2 其他靶点 纯度
Piroxicam 98%
Salicylic acid 98%
Phenacetin 98%
Etodolac 99%
Flunixin meglumine 98%
Ibuprofen L-lysine 98%
Nabumetone 98%
Acemetacin 98%
Diflunisal 98%
Pranoprofen 98%
Ampiroxicam 98%
Meloxicam 98%
Sulindac 98%
Ketoprofen 98%
Mefenamic Acid 95%
Bromfenac sodium 98%
Oxaprozin 99%
Aspirin 99%
Nepafenac 98%
Zaltoprofen 99%
Salicin 98%
Suprofen 99%+
Xanthohumol 99%
Parecoxib 98%
Tolfenamic Acid +++

COX-2, IC50: 0.2 μM

98%
Etoricoxib 99%
Niflumic Acid 98%
Valdecoxib ++++

COX-2, IC50: 5 nM

99+%
Ibuprofen +

COX-1, IC50: 13 μM

+

COX-2, IC50: 370 μM

98%
Indomethacin ++

COX1, IC50: 0.28 μM

+

COX-2, IC50: 14 μM

97%
Lornoxicam ++++

COX-1, IC50: 5 nM

++++

COX-2, IC50: 8 nM

98%
Meclofenamic acid sodium ++++

COX-1, IC50: 40 nM

+++

COX-2, IC50: 50 nM

99%
Asaraldehyde 98%
Naproxen +

COX-1, IC50: 8.7 μM

+

COX-2, IC50: 5.2 μM

98%
Diclofenac Sodium Salt +++

COX-1, IC50: 60 nM

+++

COX-2, IC50: 200 nM

98%
NS-398 ++

COX-2, IC50: 3.8 μM

95%
Amfenac Sodium Hydrate ++

COX-1, IC50: 250 nM

+++

COX-2, IC50: 150 nM

98%+
Nimesulide +

COX-2, IC50: 26 μM

98%
Lumiracoxib ++

COX-1, Ki: 3 μM

+++

COX-2, Ki: 60 nM

98%
Rutaecarpine 95%
Celecoxib ++++

COX-2, IC50: 40 nM

98%
Carprofen ++++

canine COX2, IC50: 30 nM

98%
Ketorolac ++

COX-1 (human), IC50: 1.23 μM

++

COX-2 (human), IC50: 3.50 μM

98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Tolfenamic Acid/托灭酸 生物活性

靶点
  • COX-2

    COX-2, IC50:0.2 μM

描述 Tolfenamic Acid is a nonsteroidal antiinflammatory 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[3]. Tolfenamic Acid also acts as a potent Sp protein inhibitor. Tolfenamic acid (TA) inhibits cancer cell proliferation and tumor growth through the degradation of Sp1, Sp3, and Sp4. Tolfenamic Acid (50 mg/kg 3 times/wk, p.o.) inhibits tumor formation and tumor incidence in N-nitrosomethylbenzylamine (NMBA)-induced esophageal tumor model. Tolfenamic Acid also causes decreases in tumor multiplicity and tumor volume in rats treated with NMBA[4]. Tolfenamic Acid (50 μM) significantly affects gene expression in L3.6pl cells, and downregulates CENPF, KIF20A, LMNB1, MYB, SKP2, CCNE2, and DDIT3[5]. TA has shown excellent in vitro antibacterial activity against certain ATCC strains of bacteria when complexed with bismuth(III) [6].

Tolfenamic Acid/托灭酸 细胞实验

Cell Line
Concentration Treated Time Description References
FG cells 2.5, 5.0, 10.0, 20.0, 40.0 μM TA 24-48 hours To evaluate the cytotoxicity of TA on FG cells, results showed dose-dependent inhibition of cell proliferation Cancer Res. 2010 Feb 1;70(3):1111-9.
PANC-1 cells 0.05 μM MIT + 5 μM TA 12 hours To evaluate the effect of combined MIT and TA on Sp1 protein expression, results showed significant downregulation of Sp1 protein expression Cancer Res. 2010 Feb 1;70(3):1111-9.
PANC-1 cells 5, 10, 20 μM 24 hours To evaluate the effect of TA on Sp1 protein expression, results showed dose-dependent downregulation of Sp1 protein expression Cancer Res. 2010 Feb 1;70(3):1111-9.
SKBR3 cells 25-100 µM 6 days Tolfenamic acid inhibited the proliferation of SKBR3 cells with an IC50 value of 52.5 µM. Mol Cancer Ther. 2009 May;8(5):1207-17.
BT474 cells 25-100 µM 6 days Tolfenamic acid inhibited the proliferation of BT474 cells with an IC50 value of 41.5 µM. Mol Cancer Ther. 2009 May;8(5):1207-17.
RD cells 100 μM 24 or 48 hours Inhibited cell proliferation and migration, induced apoptosis Int J Cancer. 2013 Feb 15;132(4):795-806.
RH30 cells 75 μM 24 or 48 hours Inhibited cell proliferation and migration, induced apoptosis Int J Cancer. 2013 Feb 15;132(4):795-806.
Schistosoma mansoni adult worms 50 μM 72 hours Evaluation of the schistosomicidal effect of Tolfenamic Acid on adult worms, LC50 of 20.6 μM. EBioMedicine. 2019 May;43:370-379.
SH-SY5Y cells 25 µM 72 hours To evaluate the inhibitory effects of TA and its analogs TN3 and TN7 on SP1-DNA binding. Results showed that TA, TN3, and TN7 all reduced SP1-DNA binding. Int J Mol Sci. 2023 Oct 16;24(20):15216.
SH-SY5Y neuroblastoma cells 25 μM and 50 μM 48 hours and 96 hours To investigate the effects of tolfenamic acid on Pb-induced SP1, APP, and Aβ levels. Results showed that tolfenamic acid significantly reduced Pb-induced SP1, APP, and Aβ levels. Neuropharmacology. 2014 Apr;79:596-602.
H9C2 myoblasts 50 μM 6 hours Inhibition of SP1 to mitigate Aβ-induced cell death and cardiomyocyte contractile dysfunction Acta Pharmacol Sin. 2022 Jan;43(1):39-49.

Tolfenamic Acid/托灭酸 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Athymic nude mice BT474 cell mammary fat pad xenograft model Oral gavage 25 mg/kg/d Once daily for 27 days Tolfenamic acid significantly inhibited the growth of BT474 cell xenografts and reduced tumor weight. Mol Cancer Ther. 2009 May;8(5):1207-17.
Athymic nude mice RH30 cell xenograft model Oral gavage 50 mg/kg/dose Every second day for 20 days Inhibited tumor growth, downregulated Sp1, Sp3, Sp4 and Sp-regulated genes Int J Cancer. 2013 Feb 15;132(4):795-806.
APP YAC transgenic mice Alzheimer's disease model Oral gavage 5 mg/kg and 50 mg/kg Once daily for 34 days To investigate the effects of tolfenamic acid on BACE1 gene expression and enzyme activity. Results showed that tolfenamic acid significantly reduced BACE1 gene expression and enzyme activity. Neuropharmacology. 2014 Apr;79:596-602.
Female Swiss mice Schistosoma mansoni infection model Oral 400 mg/kg single dose Single dose Evaluation of the schistosomicidal effect of Tolfenamic Acid on adult worms in mice, worm burden reduction of 62.4%. EBioMedicine. 2019 May;43:370-379.
Transgenic mice Alzheimer's disease model Oral gavage 5 or 50 mg/kg Once daily for 34 days Tolfenamic acid lowers tau mRNA and protein, as well as the levels of its phosphorylated form and CDK5. J Neurochem. 2015 Apr;133(2):266-72
Mice AD transgenic mouse model Oral gavage 5 and 50 mg/kg/day Daily administration for 34 days To evaluate the cognitive improvement effects of tolfenamic acid, results showed that 50 mg/kg/day dose significantly improved long-term and working memory deficits. Neurobiol Aging. 2013 Oct;34(10):2421-30
Nude mice PANC-1 xenograft model Oral gavage 10 mg/kg Twice a week for 45 days To evaluate the effect of TA alone on tumor growth, results showed marginal antitumor activity at low doses Cancer Res. 2010 Feb 1;70(3):1111-9.

Tolfenamic Acid/托灭酸 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
NCT02159248 Pancreatic Cancer Phase 1 Withdrawn(The study closed pri... 展开 >>or to enrolling any participants.) 收起 << December 2019 United States, Florida ... 展开 >> UF Health Cancer Center at Orlando Health Orlando, Florida, United States, 32806 收起 <<

Tolfenamic Acid/托灭酸 参考文献

[1]Sankpal UT, Goodison S, et al. Tolfenamic acid-induced alterations in genes and pathways in pancreatic cancer cells. Oncotarget. 2017 Feb 28;8(9):14593-14603.

[2]Lee SH, Bahn JH, et al. ESE-1/EGR-1 pathway plays a role in tolfenamic acid-induced apoptosis in colorectal cancer cells. Mol Cancer Ther, 2008. 7(12): p. 3739-50.

[3]Kay-Mugford P, Benn SJ, LaMarre J, Conlon P. In vitro effects of nonsteroidal anti-inflammatory drugs on cyclooxygenase activity in dogs. Am J Vet Res. 2000;61(7):802-810

[4]Maliakal P, Abdelrahim M, Sankpal UT, et al. Chemopreventive effects of tolfenamic acid against esophageal tumorigenesis in rats. Invest New Drugs. 2012;30(3):853-861

[5]Sankpal UT, Goodison S, Jones-Pauley M, Hurtado M, Zhang F, Basha R. Tolfenamic acid-induced alterations in genes and pathways in pancreatic cancer cells. Oncotarget. 2017;8(9):14593-14603

[6]Ahmed S, Sheraz MA, Ahmad I. Tolfenamic Acid. Profiles Drug Subst Excip Relat Methodol. 2018;43:255-319

Tolfenamic Acid/托灭酸 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.82mL

0.76mL

0.38mL

19.11mL

3.82mL

1.91mL

38.21mL

7.64mL

3.82mL

Tolfenamic Acid/托灭酸 技术信息

CAS号13710-19-5
分子式C14H12ClNO2
分子量 261.7
SMILES Code O=C(O)C1=CC=CC=C1NC2=CC=CC(Cl)=C2C
MDL No. MFCD00133865
别名 托芬那酸 ;GEA 6414; Clotam
运输蓝冰
InChI Key YEZNLOUZAIOMLT-UHFFFAOYSA-N
Pubchem ID 610479
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry, room temperature

溶解方案

DMSO: 105 mg/mL(401.22 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的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
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