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Niflumic acid
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Niflumic acid图片
CAS NO:4394-00-7
规格:≥98%
包装与价格:
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

产品介绍
理化性质和储存条件
Molecular Weight (MW)282.22
FormulaC13H9F3N2O2
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

实验参考方法
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.