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                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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| Type | HazMat fee for 500 gram (Estimated) | 
| Excepted Quantity | USD 0.00 | 
| Limited Quantity | USD 15-60 | 
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| Inaccessible (Haz class 6.1), International | USD 150+ | 
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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。 | |||||||||||||||||||
| 靶点 | 
 | 
| 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]. | 
| 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. | 
| 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. | 
| 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 << | 
| 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 | |
| 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 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 
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