Celecoxib

ArtNr	S1261-100
Hersteller	Selleckchem
CAS-Nr.	169590-42-5
Menge	100 mg
Quantity options	100 mg 1 g 10 g 10 mM/1 mL 5 g
Kategorie	Oncology Neuroscience Aging & Neurological Disorders Cardiovascular Research Thrombosis & Hemostasis Atherosclerosis Inhibitors & Compound Libraries Small Molecules By Organ Head & Neck Cancer
Typ	Inhibitors
Specific against	other
Smiles	CC1=CC=C(C=C1)C2=CC(=NN2C3=CC=C(C=C3)S(=O)(=O)N)C(F)(F)F
ECLASS 10.1	32160490
ECLASS 11.0	32160490
UNSPSC	12000000
Alias	SC 58635
Similar products	Celecoxib
Lieferbar
Manufacturer - Targets	MT-CO1
Storage Conditions	2 years -80 in solvent
Molecular Weight	381, 37
Administration	Administered via p.o.
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 uL of mineral oil is administered to the right hind foot pad of male Sprague Dawley rats.
Cell lines	HNE1 and CNE1-LMP1
Clinical Trials	Celecoxib is currently in Phase II clinical trials in patients with recurrent respiratory papillomatosis.
Concentrations	0-75 uM
Dosages	<=200 mg/kg
Formulation	Celecoxib is dissolved in 0.5% methyl cellulose and 0.025% Tween-20.
IC50	40 nM [1], 40 nM [1], 40 nM [1], 40 nM [1], 40 nM [1], 40 nM [1]
In vitro	Celecoxib shows low sensitivity against COX-1 with IC50 of 15 uM. [1], Celecoxib shows an anti-proliferative effect on nasopharyngeal carcinoma (NPC) cell lines including HNE1 and CNE1-LMP1 with IC50 of 32.86 uM and 61.31 uM, 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]
Incubation Time	48 hours
Kinase Assay	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 uM). 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 ug of protein) for 10 minutes before addition of arachidonic acid. PGE2 formed is detected by ELISA after 10 minute incubation.
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 uM) dissolved in DMSO (final concentration <=0.1%) and incubated for up to 48 hours. After the incubation, 20 uL 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.
Solubility (25C)	DMSO 76 mg/mL, Water <1 mg/mL, Ethanol 33 mg/mL
Information	Celecoxib is a selective COX-2 inhibitor with IC50 of 40 nM in Sf9 cells.
Chemical Name	4-(5-p-tolyl-3-(trifluoromethyl)-1H-pyrazol-1-yl)benzenesulfonamide

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