For research use only.
CAS No. 530-78-9
Flufenamic Acid is an anti-inflammatory agent, and also acts as an ion channel modulator.
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|Description||Flufenamic Acid is an anti-inflammatory agent, and also acts as an ion channel modulator.|
Flufenamic acids reversibly inhibits ICl(Ca) in Xenopus oocytes with IC50 of 28 mM, elicit in response to depolarizing voltage steps, in a dose-dependent manner, with no effect on the shape of the current-voltage curve.  Flufenamic acids blocks Ca2(+)-activated non-selective cation channels in inside-out patches from the basolateral membrane of rat exocrine pancreatic cells with IC50 of 10 μM.  Flufenamic acid binds with high affinity and negative cooperativity (pH 7.6) to wild-type (KD1=30 nM, KD2=255 nM), V30M (KD1=41 nM, KD2=320 nM) and L55P transthyretin (KD1=74 nM, KD2=682 nM), completely inhibiting amyloid fibril formation at a concentration of 10.8 μM, 3× the physiological concentration of transthyretin (3.6 μM), under conditions where transthyretin amyloid fibril formation is maximal (pH 4.4).  Flufenamic acid (viz 200 μM) produces a near complete collapse of the holding current at −50 mV, mirroring the effect of removal of extracellular Ca2+. Flufenamic acid inhibits recombinant human TRPM2 (hTRPM2) as well as currents activated by intracellular ADP-ribose in the CRI-G1 rat insulinoma cell line. Flufenamic acid antagonises ADP-ribose activated currents in the rat insulinoma cell line CRI-G1 in concentration- and pH-dependent kinetics manner.  Flufenamic acid reversibly inhibits (IC50 = 13.8 μM) DAPs and phasic firing with a similar time course in rat supraoptic neurones, but has no significant effects (P > 0.05) on membrane potential, spike threshold and input resistance, nor on the frequency and amplitude of spontaneous synaptic potentials. 
-  White MM, et al. Mol Pharmacol, 1990, 37(5), 720-724.
-  Gögelein H, et al. FEBS Lett, 1990, 268(1), 79-82.
-  Baures PW, et al. Bioorg Med Chem, 1999, 7(7), 1339-1347.
|In vitro||DMSO||56 mg/mL (199.12 mM)|
|Ethanol||56 mg/mL (199.12 mM)|
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