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2-(3-Trifluoromethylanilino)benzoic Acid/氟芬那酸 {[allProObj[0].p_purity_real_show]}

货号:A416271 同义名: 氟灭酸 / Flufenamic acid; CI-440

2-(3-Trifluoromethylanilino)benzoic Acid是一种COX抑制剂,通过防止前列腺素的形成,结合并减少前列腺素F合酶的活性,激活TRPC6,是一种非甾体抗炎药(NSAID)。

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There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.

Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
Limited Quantity USD 15-60
Inaccessible (Haz class 6.1), Domestic USD 80+
Inaccessible (Haz class 6.1), International USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic USD 100+
Accessible (Haz class 3, 4, 5 or 8), International USD 200+
2-(3-Trifluoromethylanilino)benzoic Acid/氟芬那酸 化学结构 CAS号:530-78-9
2-(3-Trifluoromethylanilino)benzoic Acid/氟芬那酸 化学结构
CAS号:530-78-9
2-(3-Trifluoromethylanilino)benzoic Acid/氟芬那酸 3D分子结构
CAS号:530-78-9
2-(3-Trifluoromethylanilino)benzoic Acid/氟芬那酸 化学结构 CAS号:530-78-9
2-(3-Trifluoromethylanilino)benzoic Acid/氟芬那酸 3D分子结构 CAS号:530-78-9
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2-(3-Trifluoromethylanilino)benzoic Acid/氟芬那酸 纯度/质量文件 产品仅供科研

货号:A416271 标准纯度: {[allProObj[0].p_purity_real_show]}
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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。

2-(3-Trifluoromethylanilino)benzoic Acid/氟芬那酸 生物活性

描述 Flufenamic acid is a non-steroidal anti-inflammatory agent, inhibits cyclooxygenase (COX), and also modulates ion channels, blocking chloride channels and L-type Ca2+ channels, modulating non-selective cation channels (NSC), activating K+ channels. Flufenamic acid inhibits a wide spectrum of TRP channels, including: C3, C7, M2, M3, M4, M5, M7, M8, V1, V3, and V4 but activates at least two TRP channels (C6 and A1)[3]. Flufenamic acid (FFA) has previously been demonstrated to be a potent activator of AMP-activated protein kinase (AMPK), which is a negative regulator of NF-κB signaling. In a mouse closed loop model of EL infection, FFA treatment (20mg/kg) significantly abrogated EL-induced intestinal fluid secretion and barrier disruption. In addition, FFA suppressed NF-κB nuclear translocation and expression of proinflammatory mediators and promoted AMPK phosphorylation in the EL-infected mouse intestine. Furthermore, FFA promoted tight junction assembly and prevented interferon gamma (IFN-γ)-induced barrier disruption in an AMPK-dependent manner[4]. FFA inhibited cAMP-dependent Cl- secretion in T84 cell monolayers with IC50 of ∼8 μM. FFA inhibited Ca2+-dependent Cl- secretion with IC50 of ∼10 μM. FFA inhibited activities of Ca2+-activated Cl- channels and KCa3.1, a Ca2+-activated basolateral K+ channels, but had no effect on activities of Na+-K+-Cl- cotransporters and Na+-K+ ATPases[5].

2-(3-Trifluoromethylanilino)benzoic Acid/氟芬那酸 细胞实验

Cell Line
Concentration Treated Time Description References
Pig ventricular myocytes 100 µM >5 minutes Investigate the effect of FFA on membrane ion currents, FFA caused an increase in currents with a reversal potential of +38 mV Br J Pharmacol. 2010 Sep;161(2):416-29.
Mouse precursor osteoblasts (D1 cells) 1.0 and 2.0 mg/mL 21 days Investigate the effect of FA on the proliferation and mineralization of D1 cells. Results showed that high concentrations of FA were not conducive to the proliferation of D1 cells but enhanced mineralization activity. Pharmaceuticals (Basel). 2023 May 1;16(5):680.
Primary microglial cells 100 µM 24 hours FA suppressed Syk activation, restored AMPK activity, and improved mitochondrial fission/fusion balance. Aging Cell. 2022 May;21(5):e13623.
Primary microglial cells 200 µM 24 hours FA inhibited microglial NLRP3 inflammasome activation by regulating Syk and AMPK, reducing ASC speck formation and IL-1β secretion. Aging Cell. 2022 May;21(5):e13623.
Candida albicans SC5314 strain ≥8 mg/L 24 hours Evaluate the preventive effect of FFA combined with FLU on Candida albicans biofilm formation, results showed that FFA ≥8 mg/L combined with FLU 32 mg/L could increase antifungal activity to 99% Int J Antimicrob Agents. 2014 Jan;43(1):86-91.
Candida albicans mature biofilms 1024 mg/L 24 hours Evaluate the therapeutic effect of FFA on mature Candida albicans biofilms, results showed that FFA concentrations of 1024 mg/L could reduce >85% of biofilm metabolic activity Int J Antimicrob Agents. 2014 Jan;43(1):86-91.
Candida albicans biofilms ≥512 mg/L 24 hours Evaluate the preventive effect of FFA on Candida albicans biofilm formation, results showed that FFA concentrations of ≥512 mg/L could prevent >80% of biofilm formation Int J Antimicrob Agents. 2014 Jan;43(1):86-91.
Hippocampal pyramidal neurons 200 µM 30 ms To investigate the effect of FFA on voltage-gated sodium currents, results showed that FFA inhibits ~50% of the sodium current with an IC50 of 189 μM. J Physiol. 2010 Oct 15;588(Pt 20):3869-82.
Airway smooth muscle cells (ASMCs) 100 µM 330 seconds Evaluate the relaxing effect of FFA on ASMCs, results showed FFA significantly reduced cell stiffness at 100 μM. Theranostics. 2024 Feb 17;14(4):1744-1763.
Airway smooth muscle cells (ASMCs) 1 µM 330 seconds Evaluate the relaxing effect of FFA on ASMCs, results showed FFA rapidly reduced cell stiffness at 1 μM. Theranostics. 2024 Feb 17;14(4):1744-1763.
Rat supraoptic nucleus neuroendocrine cells 0.3 mM–5 mM 5–10 minutes To examine the effects of flufenamic acid (FFA) on depolarizing afterpotentials (DAPs), results showed that FFA reversibly inhibited DAPs with an IC50 of 13.8 mM. J Physiol. 2002 Dec 1;545(2):537-42.
Human adipose-derived stem cells (hASCs) 25, 50, 100, 200 µM 7 days Low concentrations of FFA (25, 50, 100 μM) significantly enhanced osteogenic differentiation of hASCs, as evidenced by increased ALP activity and accelerated mineralization; 200 μM FFA inhibited osteogenic differentiation. The optimal concentration was 50 μM. Stem Cell Res Ther. 2019 Jul 19;10(1):213.
Human bone marrow-derived mesenchymal stem cells (hBMMSCs) 25, 50, 100, 200 µM 7 days Low concentrations of FFA (25, 50, 100 μM) significantly enhanced osteogenic differentiation of hBMMSCs, as evidenced by increased ALP activity and accelerated mineralization; 200 μM FFA inhibited osteogenic differentiation. The optimal concentration was 50 μM. Stem Cell Res Ther. 2019 Jul 19;10(1):213.
HEK293 cells 2.49 µM (IC50) 72 hours Assessed cytotoxicity, showing lower toxicity towards HEK293 cells, indicating selectivity for cancer cells over non-cancerous cells Angew Chem Int Ed Engl. 2024 Feb 5;63(6):e202317940.
HMLER-shEcad cells 0.18 µM (IC50) 72 hours Assessed cytotoxicity, showing sub-micromolar toxicity towards HMLER-shEcad cells, with 24-fold and 31-fold higher potency than salinomycin and cisplatin, respectively Angew Chem Int Ed Engl. 2024 Feb 5;63(6):e202317940.
HMLER cells 0.27 µM (IC50) 72 hours Assessed cytotoxicity, showing sub-micromolar toxicity towards HMLER cells Angew Chem Int Ed Engl. 2024 Feb 5;63(6):e202317940.

2-(3-Trifluoromethylanilino)benzoic Acid/氟芬那酸 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Mice 4T1 metastatic triple-negative breast cancer model Intraperitoneal injection 10 mg/kg Three times a week for 14 days Evaluated in vivo antitumour efficacy, showing significant inhibition of tumour growth and reduced lung metastasis without inducing significant systemic toxicity Angew Chem Int Ed Engl. 2024 Feb 5;63(6):e202317940.
C57BL/6 mice and Thy1-GFP-M mice T10 spinal cord contusion model Intraperitoneal injection 12.5 mg/kg Once daily for one week FFA inhibited Trpm4 expression, reduced secondary hemorrhage and capillary fragmentation, and promoted angiogenesis; inhibited the expression of MMP-2 and MMP-9, attenuated BSCB disruption; decreased the activation of microglia/macrophages, reduced lesion size and cavity formation, protected motor neurons, and improved locomotor function. Theranostics. 2018 Jul 30;8(15):4181-4198
C57BL/6J mice Cardiac arrest/cardiopulmonary resuscitation model Intraperitoneal injection 12.5 mg/kg Once daily for one week FFA improved survival and neurologic outcome after CA/CPR in mice, reduced neuropathological injuries, attenuated brain edema, lessened the leakage of IgG and Evans blue dye, restored tight junction protein expression, and promoted microglia/macrophages from the pro-inflammatory subtype toward the anti-inflammatory subtype. J Neuroinflammation. 2022 Sep 1;19(1):214
BALB/c mice Ovalbumin-induced asthmatic Mice model Inhalation 2, 4, 8 μg Single administration Evaluate the effect of FFA on airway resistance in vivo, results showed FFA significantly reduced airway resistance at 8 μg. Theranostics. 2024 Feb 17;14(4):1744-1763.
ADLPAPT mice Alzheimer's disease model Intraperitoneal injection 5 mg/kg Once daily for 8 weeks FA inhibited microglial NLRP3 inflammasome activation, significantly reducing amyloid plaques and phosphorylated tau pathology while improving cognitive function. Aging Cell. 2022 May;21(5):e13623.
BALB/C nude mice Heterotopic bone formation model Subcutaneous implantation 50 μM Single implantation, lasting 8 weeks 50 μM FFA promoted osteogenic differentiation of hBMMSCs in vivo, as evidenced by more newly formed bone and collagen organization. Stem Cell Res Ther. 2019 Jul 19;10(1):213.

2-(3-Trifluoromethylanilino)benzoic Acid/氟芬那酸 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
NCT03238612 Influenza A Phase 2 Recruiting October 31, 2020 Hong Kong ... 展开 >> Ivan Hung Recruiting Hong Kong, Hong Kong Contact: Ivan FN Hung, MD FRCP    852 22554049    ivanfn@gmail.com    Sub-Investigator: Kelvin To, MD FRCPath          Sub-Investigator: KY Yuen, MD FRCPath 收起 <<

2-(3-Trifluoromethylanilino)benzoic Acid/氟芬那酸 参考文献

[1]White MM, Aylwin M. Niflumic and flufenamic acids are potent reversible blockers of Ca2(+)-activated Cl- channels in Xenopus oocytes. Mol Pharmacol. 1990 May;37(5):720-4.

[2]Gogelein H, Dahlem D, et al. Flufenamic acid, mefenamic acid and niflumic acid inhibit single nonselective cation channels in the rat exocrine pancreas. FEBS Lett. 1990 Jul 30;268(1):79-82.

[3]Guinamard R, Simard C, Del Negro C. Flufenamic acid as an ion channel modulator. Pharmacol Ther. 2013;138(2):272-284

[4]Pongkorpsakol P, Satitsri S, Wongkrasant P, et al. Flufenamic acid protects against intestinal fluid secretion and barrier leakage in a mouse model of Vibrio cholerae infection through NF-κB inhibition and AMPK activation. Eur J Pharmacol. 2017;798:94-104

[5]Pongkorpsakol P, Yimnual C, Chatsudthipong V, Rukachaisirikul V, Muanprasat C. Cellular mechanisms underlying the inhibitory effect of flufenamic acid on chloride secretion in human intestinal epithelial cells. J Pharmacol Sci. 2017;134(2):93-100

2-(3-Trifluoromethylanilino)benzoic Acid/氟芬那酸 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.56mL

0.71mL

0.36mL

17.78mL

3.56mL

1.78mL

35.56mL

7.11mL

3.56mL

2-(3-Trifluoromethylanilino)benzoic Acid/氟芬那酸 技术信息

CAS号530-78-9
分子式C14H10F3NO2
分子量 281.23
SMILES Code O=C(O)C1=CC=CC=C1NC2=CC=CC(C(F)(F)F)=C2
MDL No. MFCD00002422
别名 氟灭酸 ;Flufenamic acid; CI-440; INF-1837; CN-27554; NSC 219007; NSC 82699; Fluphenamic Acid; FFA
运输蓝冰
InChI Key LPEPZBJOKDYZAD-UHFFFAOYSA-N
Pubchem ID 3371
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry,2-8°C

溶解方案

DMSO: 105 mg/mL(373.36 mM),配合低频超声助溶,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
方案 二
方案 三
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