CeleCOXib 是一种非甾体抗炎药，是选择性的COX-2抑制剂，IC50为 40 nM。

Celecoxib is a Nonsteroidal Anti-inflammatory Drug. The mechanism of action of celecoxib is as a Cyclooxygenase Inhibitor.

在大鼠中, Celecoxib（200- 600 mg/kg）不会产生急性GI毒性,每天 mg/kgCelecoxib处理大鼠,持续10天以上,不会产生GI毒性.在佐剂性关节炎模型中,Celecoxib降低慢性炎症（ED50=0.37 mg/kg）.Hargreaves 痛模型中,Celecoxib具有镇痛活性（ED50=34.5 mg/kg）.

在HNE1（IC50=32.86 μM） 和CNE1-LMP1（IC50= 61.31 μM）的鼻咽癌细胞系中,Celecoxib能够抑制细胞增殖。Celecoxib有效选择性抑制COX-1（IC50=15 μM）,COX-2（IC50为40 nM）。

COX enzyme assay in vitro: Expression of COX protein in insect cells is determined by assessing PG-synthetic capability in homogenates from cells incubated for 3 days with COX-1 or COX-2 baculovirus. Cells expressing COX-1 or COX-2 are homogenized and incubated with arachidonic acid (10 μM). COX activity is determined by monitoring PG production. No COX activity is detected in mock-infected Sf9 cells. Celecoxib are preincubated with crude 1% CHAPS homogenates (2-10 μg of protein) for 10 minutes before addition of arachidonic acid. PGE2 formed is detected by ELISA after 10 minute incubation.

The antiproliferative effect of Celecoxib on NPC cells is assessed using an MTT assay. Cells are seeded into 96-well plates and allowed to attach for 24 hours. The cells are then treated with increasing concentrations of Celecoxib (0 to 75 μM) dissolved in DMSO (final concentration ≤0.1%) and incubated for up to 48 hours. After the incubation, 20 μL of MTT dye (5 mg/mL) are added to each well and cells are incubated at 37 °C for 4 hours. After removing the supernatants, the crystals are dissolved in DMSO and the absorbance is measured at 490 nm. The half-maximal inhibitory concentration (IC50) values and the 95% confidence intervals are calculated using probit regression using SPSS 15.0 software. The experiment is performed in triplicate and repeated at least three times.(Only for Reference)

169590-42-5

C17H14F3N3O2S

381.37

塞来西布;SC 58635;塞来昔布

Ethanol:31 mg/mL (81.3 mM)
DMSO:71 mg/mL (186.2 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years