product name Celecoxib
Description: Celecoxib (also known as SC 58635) is a potent and selective COX-2 inhibitor with IC50 of 40 nM in Sf9 cells. In vitro, celecoxib not only reduced the production of PGE2 but also inhibited the downstream effects of PGE2. Celecoxib blocked migration and invasion of A549 cells increased by PGE2 in the wound healing and transwell assays.
References: J Med Chem. 1997 Apr 25;40(9):1347-65; Int J Radiat Oncol Biol Phys. 2013 Feb 1;85(2):472-6.
381.37
Formula
C17H14F3N3O2S
CAS No.
169590-42-5
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 76 mg/mL (199.3 mM)
Water: <1 mg/mL
Ethanol: 33 mg/mL (86.5 mM)
Solubility (In vivo)
2% DMSO+30% PEG 300+5% Tween 80+ddH2O: 5mg/mL
Synonyms
SC 58635
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19406927
| In Vitro |
In vitro activity: Celecoxib shows low sensitivity against COX-1 with IC50 of 15 μM. Celecoxib shows an anti-proliferative effect on nasopharyngeal carcinoma (NPC) cell lines including HNE1 and CNE1-LMP1 with IC50 of 32.86 μM and 61.31 μM, respectively. Kinase Assay: 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. Cell Assay: 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. |
|---|---|
| In Vivo | Celecoxib exhibits a potent, oral anti-inflammatory activity. Celecoxib reduces acute inflammation in the carrageenan edema assay and chronic inflammation in the adjuvant arthritis model with ED50 of 7.1 mg/kg and 0.37 mg/kg/day, respectively. In addition, Celecoxib also exhibits analgesic activity in the Hargreaves hyperalgesia model with ED50 of 34.5 mg/kg. Besides, Celecoxib produces no acute GI toxicity in rats at doses up to 200 mg/kg and no chronic GI toxicity in rats at doses up to 600 mg/kg/day over 10 days. In a C3Hf/KamLaw female mouse model, Celecoxib increases median survival time of 105 days (range, 79-145 days) after 13.5 Gy local thoracic irradiation (LTI) alone to 142 days (range, 94-155 days). |
| Animal model | A 0.1 mL aliquot of a 1% solution of carrageenan in 0.9% sterile saline or 1 mg of Mycobacterium butyricum in 50 μL of mineral oil is administered to the right hind foot pad of male Sprague−Dawley rats. |
| Formulation & Dosage | Dissolved in 0.5% methyl cellulose and 0.025% Tween-20; ≤200 mg/kg; p.o. administration |
| References | J Med Chem. 1997 Apr 25;40(9):1347-65; Acta Pharmacol Sin. 2012 May;33(5):682-90; Int J Radiat Oncol Biol Phys. 2013 Feb 1;85(2):472-6. |
