(S)-Naproxen
(Synonyms: 萘普生; (S)-Naproxen) 目录号 : GC14820
An NSAID and COX inhibitor
Cas No.:22204-53-1
Sample solution is provided at 25 µL, 10mM.
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(S)-Naproxen is a non-selective COX inhibitor [1,2].
Cyclooxygenase (COX) is the key enzyme required for the conversion of arachidonic acid to prostaglandins. Cyclooxygenase enzymes have been involved in diverse physiological situations and disease processes ranging from inflammation to cancer. Until now, two cyclooxygenase isoforms have been identified, COX-1 and COX-2. The COX-1 enzyme is produced constitutively (i.e., gastric mucosa) and COX-2 is inducible (i.e., sites of inflammation) [3].
(S)-Naproxen inhibited the activity of human recombinant COX-1 and -2 with the IC50 values of 0.6-4.8 μM and 2.0-28.4 μM, respectively [1]. (S)-naproxen bound tightly to Aβfibrils with the Ki value of 5.70 ± 1.31 nM against [18F]FDDNP [2]. Pretreatment with (S)-naproxen significantly reduced the specific binding of [18F]FDDNP to regions of gray matter with SPs in AD specimens [4].
References:
[1] Barnett J, Chow J, Ives D, et al. Purification, characterization and selective inhibition of human prostaglandin G/H synthase 1 and 2 expressed in the baculovirus system[J]. Biochimica et Biophysica Acta (BBA)-Protein Structure and Molecular Enzymology, 1994, 1209(1): 130-139.
[2] Laneuville O, Breuer D K, Dewitt D L, et al. Differential inhibition of human prostaglandin endoperoxide H synthases-1 and-2 by nonsteroidal anti-inflammatory drugs[J]. Journal of Pharmacology and Experimental Therapeutics, 1994, 271(2): 927-934.
[3] Dubois R N, Abramson S B, Crofford L, et al. Cyclooxygenase in biology and disease[J]. The FASEB journal, 1998, 12(12): 1063-1073.
[4] Agdeppa E D, Kepe V, Petri A, et al. In vitro detection of (S)-naproxen and ibuprofen binding to plaques in the Alzheimer’s brain using the positron emission tomography molecular imaging probe 2-(1-{6-[(2-[18 F] fluoroethyl)(methyl) amino]-2-naphthyl} ethylidene) malononitrile[J]. Neuroscience, 2003, 117(3): 723-730.
Cell experiment: | BAEC are incubated for 30 min with Naproxen (0.1 ng/mL to 1 mg/mL). Arachidonic acid (30 μM) is then added, and the cells are incubated for a further 15 min at 37°C. The medium is then removed, and radioimmunoassay is used to measure the formation of 6-keto-PGF,a, PGE2, thromboxane B2, or PGF2a[1]. |
Animal experiment: | Rats[3]To measure the analgesic effects of naproxen in a carrageenaninduced model of monoarthritis, Male Sprague–Dawley rats (n=48, 217±28 g) are randomly divided into four groups of 12 by an internally developed computer program, allowing the blind performance of the behavioral experiment. To induce hyperalgesia by inflammation, animals in groups 1B, 1C, and 1D receive a 40-μL intra-articular injection of a saline solution containing 7.5 mg/mL carrageenan in the left hind limb under isoflurane anesthesia (time=−1 h). Animals in group 1A receive no injection. After 1 h (time=0) the animals in groups 1A, 1B, 1C, and 1D receive oral doses of naproxen in saline of 0, 0, 7.5 and 30 μmol/kg, respectively. The doses and time points of measurements are selected on the basis of simulations predicting measuring a full concentration-effect relationship within the time-span of the experiment[3].Mice[2]Bleomycin (0.05 IU) is instilled intratracheally to C57BL/6 mice, which are then treated by micro-osmotic pump with vehicle, JNJ7777120 (40 mg/kg b.wt.), naproxen (21 mg/kg b.wt.), or a combination of both. Airway resistance to inflation, an index of lung stiffness, is assessed, and lung specimens are processed for inflammation, oxidative stress, and fibrosis markers[2]. |
References: [1]. Mitchell JA, et al. Selectivity of nonsteroidal antiinflammatory drugs as inhibitors of constitutive and inducible cyclooxygenase. Proc Natl Acad Sci U S A. 1993 Dec 15;90(24):11693-7. | |
| Cas No. | 22204-53-1 | SDF | |
| 别名 | 萘普生; (S)-Naproxen | ||
| 化学名 | (S)-6-methoxy-α-methyl-2-naphthaleneacetic acid | ||
| Canonical SMILES | C[C@H](C(O)=O)C1=CC=C2C=C(OC)C=CC2=C1 | ||
| 分子式 | C14H14O3 | 分子量 | 230.3 |
| 溶解度 | DMF: >25 mg/ml,DMSO: >24 mg/ml,Ethanol: >55 mg/ml,PBS pH 7.2: 1 mg/ml | 储存条件 | Room temperature |
| 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 | 4.3422 mL | 21.7108 mL | 43.4216 mL |
| 5 mM | 0.8684 mL | 4.3422 mL | 8.6843 mL |
| 10 mM | 0.4342 mL | 2.1711 mL | 4.3422 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