Naproxen Sodium
(Synonyms: 萘普生钠) 目录号 : GC17975
Naproxen sodium 是一种 COX-1 和 COX-2 抑制剂，在细胞试验中 IC50 分别为 8.72 和 5.15 μM。
Cas No.:26159-34-2
Sample solution is provided at 25 µL, 10mM.
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Naproxen sodium is a nonselective cyclooxygenase inhibitor [1], with an ex vivo IC50 value of 35.48 μmol/L to cyclooxygenase-1 (COX-1) inhibition regarding naproxen plasma levels, and an ex vivo IC50 value of 64.62 µmol/L to cyclooxygenase-2 (COX-2) regarding naproxen plasma levels [2].
COX enzymes showed to be important for satellite cell fusion, proliferation and differentiation. COX-2 inhibition alone produced decreased satellite cell proliferation. Inhibition of both COX-1 and COX-2 decreased the fusion and differentiation of satellite cell [1].
Treatment with naproxen (0.5-1.5 mM) or licofelone (100-150 µM) was applied. After 48 h, the evaluation of HCA-7 cell viability was determined with trypan blue exclusion assay. Naproxen significantly decreased HCA-7 cell viability with an IC50 value of 1.45 ± 0.07 mM, and licofelone with an IC50 value of 72 ± 3.6 µM [3].
In four volunteers, 220 mg naproxen sodium b.i.d. was applied for 7 days. After a single dose and at steady state, maximal inhibition was as follows: 79% and 85% (COX-2), 94% and 93% (COX-1). In 2 of 4 volunteers applied with a single-dose administration, a greater than 95% COX-1 inhibition was transiently found at the time of maximal plasma concentration. In 1 of 4 volunteers throughout the 12-hour dose interval, a greater than 95% COX-1 inhibition was transiently found at steady state [2].
Treatments with placebo (PL) for 3 months or naproxen sodium (Nxs) 550 mg twice each day by mouth was applied to forty women suffering from Menstrual Migraine (MM). In the next 3 months, in an open study, active drug was applied to all the women. Compared to PL, treatment with Nxs significantly reduced the number of days of headache, the headache duration and intensity, and the analgesic consumption [4].
References:
[1]. Mendias CL, Tatsumi R and Allen RE. Role of cyclooxygenase-1 and -2 in satellite cell proliferation, differentiation, and fusion. Muscle Nerve, 2004, 30(4):497-500.
[2]. Hinz B, Cheremina O, Besz D, et al. Impact of naproxen sodium at over-the-counter doses on cyclooxygenase isoforms in human volunteers. Int J Clin Pharmacol Ther, 2008, 46(4):180-6.
[3]. Sances G, Martignoni E, Fioroni L, et al. Naproxen sodium in menstrual migraine prophylaxis: a double-blind placebo controlled study. Headache, 1990, 30(11):705-9.
[4]. Tavolari S, Bonafè M, Marini M, et al. Licofelone, a dual COX/5-LOX inhibitor, induces apoptosis in HCA-7 colon cancer cells through the mitochondrial pathway independently from its ability to affect the arachidonic acid cascade. Carcinogenesis, 2008, 29(2):371-80.
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. | 26159-34-2 | SDF | |
| 别名 | 萘普生钠 | ||
| 化学名 | sodium (S)-2-(6-methoxynaphthalen-2-yl)propanoate | ||
| Canonical SMILES | C[C@@](C([O-])=O)([H])C1=CC2=CC=C(OC)C=C2C=C1.[Na+] | ||
| 分子式 | C14H13NaO3 | 分子量 | 252.24 |
| 溶解度 | ≥ 6.3mg/mL in Water | 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 | 3.9645 mL | 19.8224 mL | 39.6448 mL |
| 5 mM | 0.7929 mL | 3.9645 mL | 7.929 mL |
| 10 mM | 0.3964 mL | 1.9822 mL | 3.9645 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