Ibuprofen (Advil) is a non-selective COX inhibitor with an IC50 of 0.33 mM. It is known to have an antiplatelet effect, though Ibuprofen (Advil) is relatively mild and short-lived when compared with that of aspirin or other better-known antiplatelet agents. Ibuprofen, indomethacin, and meclofenamate were potent inhibitors of the microsomal cyclooxygenase prepared from feline lung with IC50 of 0.33 mM, 29 μM, and 4.7 μM, respectively.
|Cell lines||Bladder epithelial cell line T24, RT-4 transitional cell papilloma bladder cell line, 5637 primary carcinoma bladder cell line, HCT-116, MDAMB231, MCF7, HEK293, A549, SKOV3 and DU145|
|Preparation method||Incubating each cell line with Ibuprofe of various concentrations for 48 hours. Estimating cell survival by the MTT assay, and cell death is determined by Hoechst staining used to distinguish between intact cell nuclei and fragmented nuclei undergoing cell death. Using western blotting for detection of the p75NTR protein to lysing and analyzing the cells .|
|Concentrations||Dissolved in DMSO at a concentration of 200 mM for making the stock solution, final concentration ~2 mM|
|Incubation time||48 hours|
|Animal models||Female Sprague-Dawley rats with joint inflammation induced by high-repetition and high-force (HRHF) tasks|
|Formulation||Dissolved in DMSO and diluted in saline|
|Administration||Taken orally every day|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|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.
|Solubility||DMSO 40 mg/mL|
|Related COX Products|
NS 398 is a cyclooxygenase-2 (COX-2) inhibitor.
Vitamin E is a fat-soluble vitamin with potent antioxidant properties. It is a potent peroxyl radical scavenger and inhibits noncompetitively cyclooxygenase activity in many tissues, also inhibits angiogenesis and tumor dormancy through suppressing vascular endothelial growth factor (VEGF) gene transcription.
Tenoxicam is a good HO. radicals scavenger with an IC50 of 56.7 μM.
Suprofen is a dual COX-1/COX-2 inhibitor, used as a non-steroidal anti-inflammatory analgesic and antipyretic.
Salicylic acid is a beta hydroxy acid that occurs as a natural compound in plants which is an inhibitor of ethylene biosynthesis and cyclooxygenase activity.
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