Celecoxib Licensed by Pfizer

Celecoxib is a selective COX-2 inhibitor with IC50 of 40 nM.

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Celecoxib Chemical Structure

Celecoxib Chemical Structure
Molecular Weight: 381.37

Validation & Quality Control

Customer Reviews(1)

Quality Control & MSDS

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Product Description

Biological Activity

Description Celecoxib is a selective COX-2 inhibitor with IC50 of 40 nM.
Targets COX-2 [1]
IC50 40 nM
In vitro Celecoxib shows low sensitivity against COX-1 with IC50 of 15 μM. [1] 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. [2]
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. [1] 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). [3]
Features

Protocol(Only for Reference)

Kinase Assay: [1]

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.

Cell Assay: [2]

Cell lines HNE1 and CNE1-LMP1
Concentrations 0-75 μM
Incubation Time 48 hours
Method 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.

Animal Study: [1]

Animal Models 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 Celecoxib is dissolved in 0.5% methyl cellulose and 0.025% Tween-20.
Dosages ≤200 mg/kg
Administration Administered via p.o.
Solubility 0.5% methylcellulose/0.2% Tween 80, , 30 mg/mL
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
1

References

[1] Penning TD, et al. J Med Chem, 1997, 40(9), 1347-1365.

[2] Liu DB, et al. Acta Pharmacol Sin, 2012, 33(5), 682-690.

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Clinical Trial Information( data from http://clinicaltrials.gov)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT02071303 Not yet recruiting Pain Cairo University 2014-03 Phase 2
NCT02108366 Recruiting Influenza, Human The University of Hong Kong 2014-03 Phase 3
NCT02079727 Not yet recruiting Knee Osteoarthritis IBSA Institut Biochimique SA 2014-04 Phase 3
NCT01356290 Recruiting Medulloblastoma Medical University of Vienna|Medical University of Graz|Medical University Innsbruck|General Hospital Linz|Salzburger Landeskliniken 2014-04 Phase 2
NCT02115074 Not yet recruiting Gliomas. Centre Oscar Lambret|Reliable Cancer Therapies 2014-05 Phase 1

Chemical Information

Download Celecoxib SDF
Molecular Weight (MW) 381.37
Formula

C17H14F3N3O2S

CAS No. 169590-42-5
Storage 3 years -20℃Powder
6 months-80℃in DMSO
Synonyms SC 58635
Solubility (25°C) * In vitro DMSO 76 mg/mL (199 mM)
Water <1 mg/mL (<1 mM)
Ethanol 33 mg/mL (86 mM)
In vivo 0.5% methylcellulose/0.2% Tween 80, 30 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name 4-(5-p-tolyl-3-(trifluoromethyl)-1H-pyrazol-1-yl)benzenesulfonamide

Research Area

Customer Reviews (1)


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Rating
Source Br J Pharmacol, 2014, 171(2):498-508. Celecoxib purchased from Selleck
Method Metabolic evaluation
Cell Lines Wild-type and EC-AMPK mice
Concentrations 50 mg·kg−1 ·day−1
Incubation Time 4 weeks
Results The treatment with either drug had no effects on body weight and blood glucose levels (A), but significantly decreased the circulating triglyceride and cholesterol levels in EC-AMPK mice (B).

Product Citations (2)

Tech Support & FAQs

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