| Name | Ketorolac tromethamine salt |
| Description | Ketorolac tromethamine salt (Ketorolac tris salt) non-selective inhibits the enzymes cyclooxygenase 1 (COX-1) and COX-2with anti-inflammatory, analgesic, and antipyretic activities. |
| Cell Research | Human osteoblasts cells are exposed to Ketorolac for 24 hours. Thymidine incorporation is assessed by the TopCount Microplate Scintillation and Luminescence Counters through adding [3H]-thymidine to cultures 4 hours prior to harvesting. Cell cycle distribution is determined by using propidium iodide in flow cytometer, and cell apoptosis or necrosis is detected using the Annexin V-FITC Apoptosis Detection Kit. (Only for Reference) |
| Kinase Assay | Inhibition of Prostaglandin Formation: Recombinant COX-1 and COX-2 from rat (rCOX) and human (hCOX) expressed in a baculovirus system are purified and reconstituted with 2 mM phenol and 1 μM hematin. Then the cyclooxygenase activity is measured using a radiometric assay, and the specific activity of the final enzyme preparations used is between 20,000 and 35,000 units. Ketorolac (2 -15 μL) are diluted in DMSO and preincubated with the appropriate recombinant COX (3 -15 ng) at a final concentration of 0.01 to 1000 μM in a reaction mixture (150 μL) containing 50 mM Tris-HCl buffer (pH 7.9), 2 mM EDTA, 10% glycerol, 2 mM phenol, and 1 μM hematin for 10 minutes. The reaction is initiated by addition of [14C]arachidonic acid (50–60 mCi/mmol in a final concentration of 20 μM) and is terminated 45 seconds later by the addition of 100 μL of 0.2 N HCl and 750 μL of distilled water. The total reaction volume is then applied to a 1 mL C18 Sep-pak column that has previously been washed with 2 mL of methanol followed by 5 mL of deionized water. Oxygenated products are eluted with 3 mL of a mixture of acetonitrile/water/acetic acid (50:50:0.1, v/v/v) and quantified by liquid scintillation spectroscopy. |
| In vitro | In models of acetic acid-induced writhing (ID50=0.24 mg/kg), carrageenan-induced hyperalgesia in the paw (ID50=0.29 mg/kg), and carrageenan-induced rat paw edema (ID50=0.08 mg/kg), (R,S)-Ketorolac has demonstrated efficacy. |
| In vivo | Ketorolac inhibits prostaglandin synthesis in HEL cells (COX-1) (IC50=0.025 μM) and LPS-stimulated Mono Mac 6 cells (COX-2) (IC50=0.039 μM). In human osteoblasts (hOB), Ketorolac dose-dependently suppresses thymidine incorporation and proliferation at the G0/G1 phase, blocking cell cycle progression. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 65 mg/mL (172.69 mM)
H2O : 14 mg/mL (37.2 mM)
Ethanol : 70 mg/mL (186 mM)
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| Keywords | Cyclooxygenase | RS37619 | RS-37619 | Ketorolac tromethamine | Ketorolac tromethamine salt | Inhibitor | inhibit | Ketorolac tris | RS 37619 | COX | Ketorolac |
| Inhibitors Related | Ibuprofen | Acetaminophen | Diclofenac Potassium | Paradol | Indomethacin sodium hydrate |
| Related Compound Libraries | Anti-Neurodegenerative Disease Compound Library | Bioactive Compound Library | Inhibitor Library | FDA-Approved Drug Library | Bioactive Compounds Library Max | Anti-Cancer Drug Library |
United States
