奥沙普秦 T0708

Product Introduction
Bioactivity


英文名: Oxaprozin

描述: Oxaprozin (Oxaprozinum) 是 COX-1和 COX-2的抑制剂，还能抑制 NF-κB 的活化，对人类血小板 COX-1 和 IL-1 刺激的人类滑膜细胞 COX-2 的 IC50值分别为 2.2 和 36 μM。

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

溶解度: Ethanol : 26 mg/mL (88.6 mM)
DMSO : 55 mg/mL (187.5 mM)


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: Micheliolide | Deoxyelephantopin | Phyllanthin | Sodium 4-aminosalicylate dihydrate | Chrysotoxine | 8alpha-Hydroxyhirsutinolide | 1-Isomangostin | Bisacurone | Anti-inflammatory agent 60 | Zedoarondiol

相关库: FDA-Approved Drug Library | Drug Repurposing Compound Library | Anti-Neurodegenerative Disease Compound Library | Approved Drug Library | Anti-Cancer Drug Library | Clinical Compound Library | Anti-Cancer Clinical Compound Library | Inhibitor Library | Anti-Cancer Approved Drug Library | Bioactive Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途