Oxaprozin
(Synonyms: 奥沙普秦; Oxaprozinum; Wy21743) 目录号 : GC12114
An NSAID and COX inhibitor
Cas No.:21256-18-8
Sample solution is provided at 25 µL, 10mM.
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Oxaprozin is an inhibitor of both COX-1 and COX-2 with IC50s of 2.2 μM and 36 μM for human platelet COX-1 and IL-1-stimulated human synovial cell COX-2, respectively. Oxaprozin also inhibits the activation of NF-κB.
Oxaprozin induces apoptosis in a dose-dependent manner. Oxaprozin increases caspase-3 activity in the activated but not in the resting condition. NF-κB activation is inhibited by 50 μM Oxaprozin. Oxaprozin inhibits activation of the IKK system induced by the reagent IκBα[1]. Oxaprozin dose dependently increase CD40L-treated monocyte apoptosis. 100 μM Oxaprozin induces the strongest proapoptotic effect. 100 μM Oxaprozin significantly increases CD40L-treated monocyte apoptosis. Oxaprozin treatment inhibits CD40L-induced Akt and NF-κB (p65) phosphorylation[2].
References:
[1]. Ottonello L, et al. Delayed apoptosis of human monocytes exposed to immune complexes is reversed byoxaprozin: role of the Akt/IkappaB kinase/nuclear factor kappaB pathway. Br J Pharmacol. 2009 May;157(2):294-306.
[2]. Montecucco F, et al. Oxaprozin-induced apoptosis on CD40 ligand-treated human primary monocytes is associated with the modulation of defined intracellular pathways. J Biomed Biotechnol. 2009;2009:478785.
Kinase experiment: | Caspase 3 activity in the presence or absence of 200 ng/mL CD40L plus 1 μg/mL CD40L enhancer and 100 μM Oxaprozin is performed. The enzymatic activity is spectrophotometrically determined for 60 minutes at 405 nm assuming an extinction coefficient of 8.8×103 M1/cm[2]. |
Cell experiment: | Purified monocytes are resuspended at 106/mL and cultured for 48 hours. In selective experiments, cells are cultured in the presence or absence of 50 μM PD98059, 1 μM SB203580, 50 μM LY294002, 20 μM SN-50, 50 μM Ac-DEVD-CHO, different doses (5, 10, 50, 100 μM) of Oxaprozin, 100 μM ibuprofen,100 μM indomethacin, or 100 μM naproxene. Percentages of apoptotic cells are measured by both fluorescence microscope and flow cytometer[2]. |
References: [1]. Ottonello L, et al. Delayed apoptosis of human monocytes exposed to immune complexes is reversed byoxaprozin: role of the Akt/IkappaB kinase/nuclear factor kappaB pathway. Br J Pharmacol. 2009 May;157(2):294-306. | |
| Cas No. | 21256-18-8 | SDF | |
| 别名 | 奥沙普秦; Oxaprozinum; Wy21743 | ||
| 化学名 | 3-(4,5-diphenyl-1,3-oxazol-2-yl)propanoic acid | ||
| Canonical SMILES | C1=CC=C(C=C1)C2=C(OC(=N2)CCC(=O)O)C3=CC=CC=C3 | ||
| 分子式 | C18H15NO3 | 分子量 | 293.32 |
| 溶解度 | ≥ 11.3mg/mL in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.4092 mL | 17.0462 mL | 34.0925 mL |
| 5 mM | 0.6818 mL | 3.4092 mL | 6.8185 mL |
| 10 mM | 0.3409 mL | 1.7046 mL | 3.4092 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet