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Indomethacin

CAS No. : 53-86-1

MCE 站：Indomethacin

产品活性：Indomethacin (Indometacin) 是一种有效的，可透过血脑屏障的，非选择性的 COX1 和 COX2 抑制剂，在 CHO 细胞中，对人 COX-1 和 COX-2 的 IC₅₀ 值分别为 18 nM 和 26 nM。Indomethacin 通过干扰溶酶体的正常功能来破坏自噬流 (autophagic flux)。

研究领域：Immunology/Inflammation  |  Autophagy

作用靶点：COX  |  Autophagy

In Vitro: Indomethacin is a potent and nonselective inhibitor of COX1 and COX2, with IC₅₀s of 18 nM and 26 nM for human COX-1 and COX-2, respectively, in CHO cells. Indomethacin inhibits lipopolysaccharide (LPS)-induced PGE2 production (COX-2) in a human whole blood assay with a potency (IC₅₀=0.68±0.17?μM), and suppresses coagulation-induced TXB2 production (COX-1) (IC₅₀=0.19±0.02?μM). Indomethacin blocks COX-1 with an IC₅₀ of 20±1?nM in U937 cell microsomes at a low arachidonic acid concentration (0.1?μM).

In Vivo: Indomethacin dose-dependently inhibits both the carrageenan-induced rat paw oedema (ED₅₀, 2.0?mg/kg), hyperalgesia (ED₅₀, 1.5?mg/kg), and is also effective at reversing LPS-induced pyrexia in rats (ED₅₀, 1.1?mg/kg). Indomethacin (2.5 mg/kg, i.p) decreases the number of NeuN⁺ cells in the animals at 8 days after ET-1 injection. Indomethacin also reduces microglia/macrophage activation at 14 days. Indomethacin significantly increases the number of SVZ DCX⁺ cells/field at 14 days post stroke. Indomethacin (22.9 mg/kg, p.o.) produces 8 to 10 linear mucosal lesions extended from the fundic to pyloric area of stomach wall.

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