名称 | Oxaprozin |
描述 | Oxaprozin (Oxaprozinum) is a Nonsteroidal Anti-inflammatory Drug. The mechanism of action of oxaprozin is as a Cyclooxygenase Inhibitor. The chemical classification of oxaprozin is Nonsteroidal Anti-inflammatory Compounds. |
激酶实验 | 9L cells are treated with drug for the times indicated in each experiment. Floating and attached cells are collected, pooled, resuspended in lysis buffer (10 mM HEPES buffer, pH 7.4, containing 2 mM EDTA, 0.1% CHAPS detergent, 5 mM DTT, 350 ng/mL phenylmethylsulfonyl fluoride, 10 ng/mL pepstatin A, 10 ng/mL aprotinin, and 20 ng/mL leupeptin) and lysed by three freeze-thaw cycles (alternating between a dry ice isopropanol bath and a 37°C water bath). Lysates are spun in a bench top centrifuge at full speed for 15 min and the supernatant (cell extract) fraction transferred to a new tube. Cell extracts (20 μL) are assayed for caspase 9, caspase 8, and caspase 3 activity by incubation at 37°C for either 1 h (caspase 3) or 3 h (caspase 9 and caspase 8) in 500 μL of reaction buffer (10 mM HEPES, pH 7.4, 2 mM EDTA, 0.1% CHAPS, and 5 mM DTT) containing 50 μM caspase form-selective substrate: Ac-LETD-AFC for caspase 8; Ac-LEHD-AFC for caspase 9; and Ac-DEVD-AMC for caspase 3. Background activity is determined for each sample as follows. Cell extracts are preincubated for 15 min at room temperature, with or without caspase form-selective inhibitor: 1 μM z-LETD-FMK for caspase 8, 1 μM z-LEHD-FMK for caspase 9, and 5 μL of Casputin for caspase 3. Caspase activity measured in the absence of inhibitor is divided by the background caspase activity measured in the presence of inhibitor. A value of 1 is subtracted from each measured activity, such that a caspase activity of 0 corresponds to no increase in the specific caspase activity with drug treatment. Fluorescence of the caspase product (excitation at 395 nm and emission at 525 nm for AFC substrates, and excitation at 380 nm and emission at 460 nm for the AMC substrate) is measured using a Shimadzu model RF-1501 spectrofluorophotometer and the manufacturer's PC-1501 software package. |
体内活性 | Oxaprozin的抗炎作用被认为是由于其抑制了血小板中阻断前列腺素合成的环氧化酶。可能是由于Oxaprozin对下丘脑有解热作用,导致外周血流的增加,血管扩张,随后热耗散。Oxaprozin对COX-2有较低的选择性,意味着对COX-1更高的选择性。 |
存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
溶解度 | Ethanol : 26 mg/mL (88.6 mM) DMSO : 55 mg/mL (187.51 mM), Sonication is recommended.
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关键字 | anti-inflammatory | NF-κB | IκB kinase | PKB | I kappa B kinase | COX | inhibit | Nuclear factor-kappaB | Cyclooxygenase | IKK | Akt | Protein kinase B | Nuclear factor-κB | Wy 21743 | Inhibitor | Wy-21743 | Apoptosis | NSAID | Oxaprozin |
相关产品 | Lidocaine hydrochloride | Diallyl disulfide | Ibuprofen | Glucosamine | Paradol | Acetaminophen | Indomethacin sodium hydrate | Diclofenac Potassium | Indole-3-carbinol | Diclofenac sodium |
相关库 | 抑制剂库 | 经典已知活性库 | 抗癌上市药物库 | 已知活性化合物库 | 抗衰老化合物库 | FDA 上市药物库 | 神经退行性疾病化合物库 | 药物功能重定位化合物库 | 抗癌临床化合物库 | 抗癌药物库 |