Flufenamic acidCAS号: 530-78-9分子式: C14H10F3NO2分子量: 281.23描述纯度储存/保存方法别名外观可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)
产品描述 | |
描述 |
Flufenamic Acid is an anti-inflammatory agent, and also acts as an ion channel modulator. |
纯度 |
>98%
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储存/保存方法 |
Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
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基本信息 | |
别名 |
氟芬那酸
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外观 |
白色至淡黄色结晶粉末
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可溶性/溶解性 |
Ethanol :56mg/mL(199.12mM)
DMSO :56mg/ml(199.13 mM) |
生物活性 | |
靶点 |
Potassium Channel
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In vitro(体外研究) |
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.
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In vivo(体内研究) |
Flufenamic acid (50 mg/kg, i.p.) has anti-inflammatory effect in a mouse model of Vibrio cholerae El Tor variant (EL)-induced diarrhea and significantly abrogates EL-induced intestinal fluid secretion and barrier disruption at 20 mg/kg. Furthermore, Flufenamic acid suppresses NF-κB nuclear translocation and expression of proinflammatory mediators and promotes AMPK phosphorylation in the EL-infected mouse intestine.
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分子结构图