塞来昔布 T0466

Product Introduction
Bioactivity


英文名: Celecoxib

描述: Celecoxib (SC 58635) 是一种非甾体抗炎药，是选择性的COX-2抑制剂，IC50为 40 nM。

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: 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）.

体内活性: 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）。

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: Ethanol : 31 mg/mL (81.3 mM)
5% DMSO+95% Saline : 3.55 mg/mL (9.31 mM, suspension)
DMSO : 60 mg/mL (157.33 mM)


关键字: inhibit | Inhibitor | COX | Celecoxib | Cyclooxygenase | SC-58635 | SC58635

相关产品: Piroxicam | Parecoxib | Cinchophen | Manassantin A | Ligustroside | Ginsenoside C-K | FK 3311 | (±)-Catechin | Nimesulide | Etodolac

相关库: FDA-Approved Drug Library | Drug Repurposing Compound Library | Anti-Neurodegenerative Disease Compound Library | FDA-Approved & Pharmacopeia Drug Library | Anti-Cancer Drug Library | Anti-Cancer Clinical Compound Library | Inhibitor Library | Anti-Cancer Approved Drug Library | EMA Approved Drug Library | Bioactive Compound Library

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