Celecoxib Licensed by Pfizer

Catalog No.S1261
5 5 3 Product Citations

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

Price Stock Quantity  
USD 97 In stock
USD 270 In stock
Bulk Inquiry

Massive Discount Available

Free Overnight Delivery on all orders over $ 500.

Celecoxib Chemical Structure

Celecoxib Chemical Structure
Molecular Weight: 381.37

Validation & Quality Control

Customer Reviews(1)

Quality Control & MSDS

Related Compound Libraries

COX Inhibitors with Unique Features

  • Pan COX inhibitor

    Naproxen Pan-COX inhibitor, COX-1, IC50=8.7 μM; COX-2, IC50=5.2 μM.

  • Most Potent COX Inhibitor

    Lornoxicam COX-1, IC50=5 nM; COX-2, IC50=8 nM.

  • FDA-approved Inhibitor

    Ibuprofen Approved by FDA for relieving pain, alleviating fever,and reducing inflammation.

  • Classic COX Inhibitor

    Ketorolac Non-selective COX inhibitor of COX-1 and COX-2 with IC50 of 1.23 μM and 3.50 μM, respectively.

Product Information

  • Compare COX Inhibitors
    Compare COX Products
  • Research Area

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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesBaboonDogMonkeyRabbitGuinea pigRatHamsterMouse
Weight (kg)121031.80.40.150.080.02
Body Surface Area (m2)0.60.50.240.150.050.0250.020.007
Km factor202012128653
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
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.

view more

Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2014-10-24)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT02260336 Recruiting Rheumatic Pain Chengdu PLA General Hospital October 2014 --
NCT02160301 Not yet recruiting Post Operative Pain Control University of North Carolina, Chapel Hill July 2014 Phase 4
NCT02192190 Recruiting Osteoarthritis, Knee Eli Lilly and Company July 2014 Phase 2
NCT02171104 Recruiting Mucopolysaccharidosis I|Mucopolysaccharidosis II|Mucopolysaccharidosis VI|Mucopolysaccharidosis VII|Hurler Syndrome|Hunter Syndrome|Maroteaux Lamy  ...more Mucopolysaccharidosis I|Mucopolysaccharidosis II|Mucopolysaccharidosis VI|Mucopolysaccharidosis VII|Hurler Syndrome|Hunter Syndrome|Maroteaux Lamy Syndrome|Sly Syndrome|Glycoprotein Metabolic Disorders|Alpha Mannosidosis|Fucosidosis|Aspartylglucosaminuria|Adrenoleukodystrophy|Peroxisomal Disorders|Osteopetrosis|Rett Syndrome|Sphingolipidosis|Gangliosidosis|Globoid Cell Leukodystrophy|Metachromatic Leukodystrophy|Niemann Pick B|Niemann Pick C Subtype 2|I-cell Disease Masonic Cancer Center, University of Minnesota July 2014 Phase 2
NCT02151448 Recruiting Malignant Neoplasm of Pancreas Metastatic to Peritoneal Surface|Malignant Peritoneal Mesothelioma|Peritoneal Carcinomatosis Pawel Kalinski|National Cancer Institute (NCI)|University  ...more Pawel Kalinski|National Cancer Institute (NCI)|University of Pittsburgh July 2014 Phase 1|Phase 2

view more

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)


Click to enlarge
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 (3)

Tech Support & FAQs

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

* Indicates a Required Field

Related COX Products

  • Meclofenamate Sodium

    Meclofenamate Sodium is a dual COX-1/COX-2 inhibitor with IC50 of 40 nM and 50 nM, respectively, used in the treatment of joint, muscular pain, arthritis and dysmenorrhea.

  • Vilazodone HCl

    Vilazodone HCl is a selective serotonin reuptake inhibitor (SSRI) and a partial agonist of 5-HT1A receptors, used for the treatment of major depressive disorder.

  • FLI-06

    FLI-06 is a novel inhibitor of Notch signaling with EC50 of 2.3 μM.

  • Diclofenac Sodium

    Diclofenac Sodium is a non-selective COX inhibitor with IC50 of 60 and 220 nM for ovine COX-1 and -2, respectively.

  • Lumiracoxib

    Lumiracoxib is a novel, selective COX-2 inhibitor with IC50 and Ki of 0.14 μM and 0.06 μM, exhibits 515-fold selectivity over COX-1. Phase 4.

  • Bufexamac

    Bufexamac is a COX inhibitor for IFN-α release with EC50 of 8.9 μM.

    Features:A specific inhibitor of class IIB histone deacetylases.

  • Ibuprofen Lysine

    Ibuprofen Lysine is a non-steroidal anti-inflammatory drug.

  • Ibuprofen

    Ibuprofen (Dolgesic) is an anti-inflammatory inhibitor targeting COX-1 and COX-2 with IC50 of 13 μM and 370 μM, respectively.

    Features:Considered a core medicine in the WHO's "WHO Model List of Essential Medicines" (a list of the minimum medical requirements for a basic healthcare system).

  • Asaraldehyde

    Asaraldehyde is a natural COX-2 inhibitor, exhibiting 17-fold selectivity over COX-1.

  • Nimesulide

    Nimesulide is a relatively COX-2 selective inhibitor with IC50 of 26 μM.

Recently Viewed Items

Tags: buy Celecoxib | Celecoxib ic50 | Celecoxib price | Celecoxib cost | Celecoxib solubility dmso | Celecoxib purchase | Celecoxib manufacturer | Celecoxib research buy | Celecoxib order | Celecoxib mouse | Celecoxib chemical structure | Celecoxib mw | Celecoxib molecular weight | Celecoxib datasheet | Celecoxib supplier | Celecoxib in vitro | Celecoxib cell line | Celecoxib concentration | Celecoxib nmr
Contact Us