酮咯酸氨丁三醇 T1212

Product Introduction
Bioactivity


英文名: Ketorolac tromethamine salt

描述: Ketorolac tromethamine salt (Ketorolac tris salt) 是一种非甾体抗炎剂，是非选择性的 COX 抑制剂，对 COX-1 和 COX-2 的IC50值分别为 20 和 120 nM。

细胞实验: 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)

激酶实验: 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.

体外活性: 在乙酸诱导的扭体（ID50=0.24 mg/kg）,角叉菜胶诱导的爪痛觉过敏（ID50=0.29 mg/kg）和角叉菜胶诱导的大鼠水肿（ID50=0.08 mg/kg）形成试验中,（R,S）-Ketorolac能够发挥功效.

体内活性: 在HEL细胞（COX-1）（IC50=0.025 μM）和LPS刺激的Mono Mac 6细胞（COX-2）（IC50=0.039 μM）中,Ketorolac抑制类花生酸形成。在人成骨细胞（hOB）中,] Ketorolac以剂量依赖性方式抑制胸苷掺入和细胞在G0 / G1期的增殖,阻滞细胞周期。

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 70 mg/mL (186 mM)
H2O : 14 mg/mL(37.2 mM)
Ethanol : 70 mg/mL (186 mM)


关键字: Cyclooxygenase | RS37619 | RS-37619 | Ketorolac tromethamine | Ketorolac tromethamine salt | Inhibitor | inhibit | Ketorolac tris | RS 37619 | COX | Ketorolac

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相关库: Anti-Neurodegenerative Disease Compound Library | Drug Repurposing Compound Library | Anti-Cancer Drug Library | Anti-Cancer Clinical Compound Library | Inhibitor Library | Anti-Colorectal Cancer Compound Library | Anti-Cancer Approved Drug Library | EMA Approved Drug Library | Nonsteroidal Anti-Inflammatory Compound Library | Bioactive Compound Library

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