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)。
HazMat Fee + 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+ |


| 规格 | 价格 | 会员价 | 库存 | 数量 | |||
|---|---|---|---|---|---|---|---|
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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。 | |||||||||||||||||||
| 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]. |
| 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. |
| 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. |
| 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 << |
| 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 |
|
| 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 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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