CAS NO: | 4394-00-7 |
规格: | ≥98% |
包装 | 价格(元) |
500mg | 电议 |
1g | 电议 |
2g | 电议 |
5g | 电议 |
10g | 电议 |
25g | 电议 |
50g | 电议 |
Molecular Weight (MW) | 282.22 |
---|---|
Formula | C13H9F3N2O2 |
CAS No. | 4394-00-7 |
Storage | -20℃ for 3 years in powder form |
-80℃ for 2 years in solvent | |
Solubility (In vitro) | DMSO: 56 mg/mL (198.4 mM) |
Water:<1 mg/mL | |
Ethanol: <1 mg/mL | |
Other info | Chemical Name: 2-[3-(trifluoromethyl)anilino]pyridine-3-carboxylic acid InChi Key: JZFPYUNJRRFVQU-UHFFFAOYSA-N InChi Code: InChI=1S/C13H9F3N2O2/c14-13(15,16)8-3-1-4-9(7-8)18-11-10(12(19)20)5-2-6-17-11/h1-7H,(H,17,18)(H,19,20) SMILES Code: O=C(C1=CC=CN=C1NC2=CC=CC(C(F)(F)F)=C2)O |
Synonyms | Flunir, Niflactol, Niflugel, Niflumic Acid, Donalgin, Nifluril |
In Vitro | In vitro activity: Niflumic acid inhibits Ca2+-activated Cl- channels with inhibition constant of 17 mM. Niflumic acid also inhibits ICl(Ca) elicited by bath application of Ca2+ to oocytes permeabilized using the Ca2+ ionophore A23187, demonstrating that the inhibition of ICl(Ca) is due to a direct interaction with the Cl- channel, rather than by interference with Ca2+ entry through voltage-dependent Ca2+ channels. Niflumic acid blocks Ca2+-activated non-selective cation channels in inside-out patches from the basolateral membrane of rat exocrine pancreatic cells with IC50 of 50 μM. Niflumic acid dose-dependently and reversibly activates large conductance calcium-activated K+ (KCa) channels. Niflumic acid produces a concentration-dependent inhibition of spontaneous transient inward current (STIC, calcium-activated chloride current) amplitude. Niflumic acid inhibits noradrenaline- and caffeine-evoked IO(Ca) with an ICM50 of 6.6 μM, i.e.is less potent against evoked currents compared to spontaneous currents. Niflumic acid voltage-dependently inhibits spontaneous transient inward current (STIC) amplitude with IC50 of 2.3 μM and 1.1 μM at -50 and +50 mV respectively. Niflumic acid inhibits not only IL-13-induced goblet cell hyperplasia but also airway hyperresponsiveness and eosinophilic infiltration. Niflumic suppresses the eotaxin levels in bronchoalveolar lavage fluids and overexpression of the MUC5AC gene, a marker of goblet cell hyperplasia, in the lung after IL-13 instillation. Niflumic acid suppresses JAK2 activation, STAT6 activation, and eotaxin expression in epithelial cells. |
---|---|
In Vivo | |
Animal model | |
Formulation & Dosage | |
References | Mol Pharmacol. 1990 May;37(5):720-4; FEBS Lett. 1990 Jul 30;268(1):79-82. |