| CAS NO: | 169590-42-5 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 250mg | 电议 |
| 500mg | 电议 |
| 1g | 电议 |
| 2g | 电议 |
| 5g | 电议 |
| 10g | 电议 |
| Molecular Weight (MW) | 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; YM177. Celecoxib; SC58635; YM-177; SC-58635; YM 177; trade name Celebrex; Xilebao. |
| 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. |
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