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Flufenamic acid

CAS No. : 530-78-9

MCE 站：Flufenamic acid

产品活性：Flufenamic acid 是一种非甾体类抗炎剂，能够抑制 COX 的活性，激活 AMPK 的活性，调节离子通道，阻滞氯离子通道 (chloride channel) 和 L-型钙离子通道 (L-type Ca²⁺ channel)，调节非选择性阳离子通道，激活钾离子通道 (K⁺ channel) 等。Flufenamic acid 与TEAD2 YBD 的中央囊袋结合，抑制 TEAD 功能和 TEAD-YAP 依赖性过程，如细胞迁移和增殖。

研究领域：Immunology/Inflammation  |  PI3K/Akt/mTOR  |  Epigenetics  |  Membrane Transporter/Ion Channel  |  Neuronal Signaling  |  Anti-infection

作用靶点：COX  |  AMPK  |  Potassium Channel  |  Chloride Channel  |  Calcium Channel  |  Parasite

In Vitro: Flufenamic acid is a non-steroidal anti-inflammatory agent, inhibits cyclooxygenase (COX), and also modulates ion channels, blocking chloride channels and L-type Ca²⁺ channels, modulating non-selective cation channels (NSC), activating K⁺ channels. Flufenamic acid inhibits a wide spectrum of TRP channels, including: C3, C7, M2, M3, M4, M5, M7, M8, V1, V3, and V4 but activates at least two TRP channels (C6 and A1). Flufenamic acid induces AMPK activation in T84 cells, and such an effect is via a direct stimulation of calcium/calmodulin-dependent protein kinase kinase beta (CaMKKβ) activity. Moreover, Flufenamic acid (FFA; 5-50 μM) dose-dependently inhibits cAMP-dependent Cl^- secretion in intact T84 cells, suppresses CFTR-mediated apical I_Cl^-, and blocks the Ca²⁺-dependent Cl^- secretion in a dose-dependent manner with IC₅₀ of appr 10 μM and near complete inhibition at 100 μM in T84 cell monolayers, but shows no effect on Na⁺-K⁺ ATPase or NKCC in T84 cells.

In Vivo: 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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