名称 | Celecoxib |
描述 | Celecoxib (SC 58635) is a non-steroidal anti-inflammatory agent, a COX-2 inhibitor (IC50=40 nM), with selectivity. Celecoxib has anti-inflammatory and analgesic activity and can be used for the treatment of osteoarthritis, rheumatoid arthritis, and acute pain. |
细胞实验 | 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) |
激酶实验 | 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. |
体外活性 | 方法:鼻咽癌 (NPC) 细胞系 HNE1 和 CNE1-LMP1 用 Celecoxib (5-75 µM) 处理 48 h,使用 MTT assay 检测细胞活力。
结果:Celecoxib 的抑制作用以剂量依赖的方式发生。Celecoxib 在 HNE1 和 CNE1-LMP1 中的平均 IC50 值分别为 32.86±1.13 µmol/L 和 61.31±4.30 µmol/L。[1]
方法:人正常肝细胞 L02 用 PA (200 µM) 和 Celecoxib (5-40 µM) 处理 24 h,使用 Western Blot 检测靶点蛋白表达水平。
结果:PA 诱导 COX-2 上调,LC3 II/I 和 p62 的蛋白质表达增加。PA和 Celecoxib 联用,COX-2 和 p62 的蛋白水平显著降低,LC3 II/I 增加。[2] |
体内活性 | 方法:为测试是否能降低放射性肺炎的死亡率,将 Celecoxib (25 mg/kg in 0.5% methyl cellulose and 0.025% Tween 20 in sterile water) 灌胃给药给局部胸部照射 (LTI) 的 C3Hf/KamLaw 小鼠。从 LTI 当天或 40 或 80 天后开始给药,每天两次,持续四十天。
结果:Celecoxib 相对于 LTI 的时间决定了疗效。只有当 Celecoxib 在 LTI 后 80 天开始使用时,死亡时间才能显著缩短,这与肺炎的表达时间相对应。对于这些小鼠,死亡率的降低被量化为治疗组与未治疗组的死亡率的风险比为 0.36。[3] |
存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
溶解度 | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 7.1 mg/mL (18.62 mM), Working solution is recommended to be prepared and used immediately. Ethanol : 31 mg/mL (81.3 mM) 2% DMSO+40% PEG300+5% Tween 80+53% H2O : 3 mg/mL, Sonication is recommended. Working solution is recommended to be prepared and used immediately. DMSO : 60 mg/mL (157.33 mM)
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关键字 | inhibit | Inhibitor | COX | Celecoxib | Cyclooxygenase | SC-58635 | SC58635 |
相关产品 | Trometamol | Revaprazan hydrochloride | Ibuprofen | Paradol | Glafenine | Acetaminophen | Indomethacin sodium hydrate | Diclofenac Potassium | Salicylamide | Diclofenac sodium |
相关库 | 抑制剂库 | 经典已知活性库 | 已知活性化合物库 | EMA 上市药物库 | 抗衰老化合物库 | FDA 上市药物库 | 药物功能重定位化合物库 | 疼痛相关化合物库 | 抗癌临床化合物库 | 抗癌药物库 |