Ketorolac (Toradol) is a non-selective COX inhibitor with IC50 of 31.5 µM and 60.5 µM for human recombinant COX-1 and COX-2, respectively. Ketorolac tromethamine is a non-steroidal anti-inflammatory agent (NSAID) in the family of heterocyclic acetic acid derivative, often used as an analgesic, antipyretic (fever reducer), and anti-inflammatory. Ketorolac tromethamine (Toradol) acts by inhibiting the bodily synthesis of prostaglandins. The primary mechanism of action responsible for ketorolac’s anti-inflammatory, antipyretic and analgesic effects is the inhibition of prostaglandin synthesis by competitive blocking of the enzyme cyclooxygenase (COX).
|Cell lines||Primary human osteoblasts cell lines|
|Preparation method||Exposing human osteoblasts cells to Ketorolac for 24 hours.Assessing thymidine incorporation by the TopCount Microplate Scintillation and Luminescence Counters through adding [3H]-thymidine to cultures 4 hours prior to harvesting. Using propidium iodide in flow cytometer to determine cell cycle distribution , and using the Annexin V-FITC Apoptosis Detection Kit to detect cell apoptosis or necrosis.|
|Concentrations||Dissolved in DMSO, final concentration ~0.1 mM|
|Incubation time||24 hours|
|Animal models||Male Wistar rats|
|Formulation||Dissolved in DMSO and diluted in saline.|
|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 70 mg/mL|
|Related COX Products|
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.
Propyphenazone is a pyrazolone derivative with anti-inflammatory, analgesic and antipyretic activity, Propyphenazone-based analogues as prodrugs and selective cyclooxygenase-2 inhibitors.
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