| 名稱 | Ketorolac tromethamine salt |
| 描述 | Ketorolac tromethamine salt (Ketorolac tris salt) non-selective inhibits the enzymes cyclooxygenase 1 (COX-1) and COX-2with anti-inflammatory, analgesic, and antipyretic activities. |
| 細(xì)胞實(shí)驗(yàn) | 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) |
| 激酶實(shí)驗(yàn) | 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. |
| 體外活性 | 在乙酸誘導(dǎo)的扭體（ID50=0.24 mg/kg）,角叉菜膠誘導(dǎo)的爪痛覺過敏（ID50=0.29 mg/kg）和角叉菜膠誘導(dǎo)的大鼠水腫（ID50=0.08 mg/kg）形成試驗(yàn)中,（R,S）-Ketorolac能夠發(fā)揮功效. |
| 體內(nèi)活性 | 在HEL細(xì)胞（COX-1）（IC50=0.025 μM）和LPS刺激的Mono Mac 6細(xì)胞（COX-2）（IC50=0.039 μM）中,Ketorolac抑制類花生酸形成。在人成骨細(xì)胞（hOB）中,] Ketorolac以劑量依賴性方式抑制胸苷摻入和細(xì)胞在G0 / G1期的增殖,阻滯細(xì)胞周期。 |
| 存儲(chǔ)條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | DMSO : 65 mg/mL (172.69 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (5.31 mM), Sonication is recommended.
H2O : 14 mg/mL (37.19 mM), Sonication is recommended.
Ethanol : 70 mg/mL (185.97 mM), Sonication is recommended.
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| 關(guān)鍵字 | RS-37619 | RS37619 | RS 37619 | Ketorolac tromethamine salt | Ketorolac tromethamine | Ketorolac tris | Ketorolac | COX-2 | COX-1 | COX |
| 相關(guān)產(chǎn)品 | Trometamol | Gallic Acid Monohydrate | Naproxen sodium | 4-Aminosalicylic acid | 5-Methylfurfural | Phenylbutazone | Indomethacin | Paradol | Acetaminophen | Diclofenac Potassium | Magnesium sulfate | Phenidone |
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