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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+
Chemical Structure| 530-78-9 Chemical Structure| 530-78-9

Structure of 530-78-9

Chemical Structure| 530-78-9

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Flufenamic Acid is a COX inhibitor and prevents formation of prostaglandins, binds to and reduce the activity of prostaglandin F synthase and activate TRPC6, it is a NSAID drug.

Synonyms: Flufenamic acid; CI-440; INF-1837

4.5 *For Research Use Only !

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Product Citations

Product Citations

Tonduru, Arun Kumar ; Maljaei, Seyed Hamed ; Adla, Santosh Kumar ; Anamea, Landry ; Tampio, Janne ; Kralova, Adela , et al.

Abstract: OATP1C1 (organic anion-transporting polypeptide 1C1) transports thyroid hormones, particularly thyroxine (T4), into human astrocytes. In this study, we investigated the potential of utilizing OATP1C1 to improve the delivery of anti-inflammatory drugs into glial cells. We designed and synthesized eight novel prodrugs by incorporating T4 and 3,5-diiodo-L-tyrosine (DIT) as promoieties to selected anti-inflammatory drugs. The prodrug uptake in OATP1C1-expressing human U-87MG glioma cells demonstrated higher accumulation with T4 promoiety compared to those with DIT promoiety or the parent drugs themselves. In silico models of OATP1C1 suggested dynamic binding for the prodrugs, wherein the pose changed from vertical to horizontal. The predicted binding energies correlated with the transport profiles, with T4 derivatives exhibiting higher binding energies when compared to prodrugs with a DIT promoiety. Interestingly, the prodrugs also showed utilization of oatp1a4/1a5/1a6 in mouse primary astrocytes, which was further supported by docking studies and a great potential for improved brain drug delivery.

Purchased from AmBeed: ; ; ; ; ; 5104-49-4 ; 22204-53-1

Alternative Products

Product Details of 2-(3-Trifluoromethylanilino)benzoic Acid

CAS No. :530-78-9
Formula : C14H10F3NO2
M.W : 281.23
SMILES Code : O=C(O)C1=CC=CC=C1NC2=CC=CC(C(F)(F)F)=C2
Synonyms :
Flufenamic acid; CI-440; INF-1837
MDL No. :MFCD00002422
InChI Key :LPEPZBJOKDYZAD-UHFFFAOYSA-N
Pubchem ID :3371

Safety of 2-(3-Trifluoromethylanilino)benzoic Acid

GHS Pictogram:
Signal Word:Danger
Hazard Statements:H301-H315-H319
Precautionary Statements:P264-P270-P280-P301+P310+P330-P302+P352-P305+P351+P338-P332+P313-P337+P313-P405-P501
Class:6.1
UN#:2811
Packing Group:

Isoform Comparison

Biological Activity

In Vitro:

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.

In Vivo:

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.

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT03238612 Influenza A Phase 2 Recruiting October 31, 2020 Hong Kong ... More >> 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 Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 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

References

 

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