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NS 398 is a selective inhibitor of cyclooxygenase-2 with IC50 value of 3.8 μM [1].

Cyclooxygenase (COX) is an enzyme that is responsible for the formation of prostaglandins, prostacyclin and thromboxane. COX-2 converts arachidonic acid (AA) to prostaglandin endoperoxide H2.

NS 398 is a selective COX-2 inhibitor and a novel anti-inflammatory agent. NS 398 inhibited COX-2 with IC50 value of 3.8 μM in a concentration-dependent way [1]. In RG/C2, AA/C1 and RR/C1 pre-malignant human colorectal adenoma cell lines, NS-398 (20 ~ 100 μM) inhibited cell proliferation and induced apoptosis. In HT29 colorectal carcinoma cell lines, NS-398 induced apoptosis. Also, NS-398 increased COX-2 protein expression. In HT29 cultures, NS-398 inhibited prostaglandin E2 secretion and COX-2 activity [2].

In rats with trauma, NS-398 (0.3-5 mg/kg) exhibited anti-inflammatory and analgesic effects [1]. In Balb/C mice, NS-398 (10 mg/kg) reduced prostaglandin E2 (PGE2) production and also significantly decreased the production of NO, IL-6 and TNF-α. Also, NS-398 decreased the mRNA levels of COX-2 and inhibited NF-κB activation. These results suggested that NS-398 regulated the inflammatory response after trauma and improved survival [3].

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