Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
50 mg | ¥ 646 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 247 | 现货 |
产品描述 | 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. |
靶点活性 | COX-1:2.2 μM, COX-2:36 μM |
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。 |
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. |
别名 | 奥沙普秦, Oxaprozinum, Wy21743 |
分子量 | 293.32 |
分子式 | C18H15NO3 |
CAS No. | 21256-18-8 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: 26 mg/mL (88.6 mM)
DMSO: 55 mg/mL (187.5 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
Ethanol / DMSO | 1 mM | 3.4092 mL | 17.0462 mL | 34.0925 mL | 85.2311 mL |
5 mM | 0.6818 mL | 3.4092 mL | 6.8185 mL | 17.0462 mL | |
10 mM | 0.3409 mL | 1.7046 mL | 3.4092 mL | 8.5231 mL | |
20 mM | 0.1705 mL | 0.8523 mL | 1.7046 mL | 4.2616 mL | |
50 mM | 0.0682 mL | 0.3409 mL | 0.6818 mL | 1.7046 mL | |
DMSO | 100 mM | 0.0341 mL | 0.1705 mL | 0.3409 mL | 0.8523 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Oxaprozin 21256-18-8 Immunology/Inflammation Neuroscience NF-Κb NF-κB COX anti-inflammatory IκB kinase PKB I kappa B kinase inhibit 奥沙普秦 Nuclear factor-kappaB Cyclooxygenase IKK Akt Protein kinase B Nuclear factor-κB Wy 21743 Inhibitor Wy-21743 Oxaprozinum Apoptosis NSAID Wy21743 inhibitor