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Etoricoxib

CAS No. : 202409-33-4

MCE 站：Etoricoxib

产品活性：Etoricoxib (MK-0663) 是一种非甾体抗炎剂，为可口服的、选择性的 COX-2 抑制剂，对人全血 COX-2 和 COX-1 的 IC₅₀ 值分别为 1.1 μM 和 116 μM。

研究领域：Immunology/Inflammation

作用靶点：COX

In Vitro: Etoricoxib (MK-0663) is a selective and orally active COX-2 inhibitor, with IC₅₀s of 1.1 μM, 116 μM and 5 μM for COX-2, COX-1 in human whole blood and purified human COX-2, respectively. Etoricoxib (MK-0663) shows inhibitory effect on PGE2 production by CHO (COX-2) cells (IC₅₀, 79 nM), on purified human COX-2 with detergent (IC₅₀, 4.1 μM), and on purified PGE2 production by U937 microsomes (low substrate; IC₅₀, 12.1 μM). However, Etoricoxib (MK-0663) has little activity against COX-1 with a K_i of 167 μM.

In Vivo: Etoricoxib (MK-0663) (0.1-30 mg/kg, p.o.) dose-dependently inhibits carrageenan-induced paw edema, carrageenan-induced paw hyperalgesia, and endotoxin-induced pyresis in rats. Etoricoxib (≥10 mg/kg) completely reverses hyperalgesia response in the rat hyperalgesia model. Etoricoxib (MK-0663) (200 mg/kg/day) has no effect on urinary ⁵¹Cr excretion in rats, and nor in monkeys at 100 mg/kg/day. Etoricoxib (MK-0663) (50 and 100?mg/kg) potently increases the malondialdehyde (MDA) and myeloperoxidase (MPO) levels, and decreases the total glutathione (tGSH) and glutathione reductase (GSHRd) levels in rats. Etoricoxib (MK-0663) (100?mg/kg) significantly inhibits the decrease of NO in rats. Etoricoxib (MK-0663) (0.64 mg/kg, p.o.) reduces the features such as multiple plaque lesions, hyperplasia and dysplasia induced by 1,2-dimethylhydrazine dihydrochloride (DMH) in rats.

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