Naproxen Sodium

製品コードS1626 バッチS162601

印刷

化学情報

Chemical Structure Synonyms RS-3650 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C14H13NaO3
分子量 252.24 CAS No. 26159-34-2
Solubility (25°C)* 体外 Water 76 mg/mL (301.3 mM)
Ethanol 15 mg/mL (59.46 mM)
DMSO 3 mg/mL (11.89 mM)
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 Naproxen Sodium (RS-3650) は、COX-1 および COX-2 の COX 阻害剤であり、それぞれ 8.7 μM および 5.2 μM の IC50 を持ちます。
in vitro Naproxen is approximately equipotent inhibitor of COX-1 and COX-2 in intact cells with IC50 of 2.2 μg/mL and 1.3 μg/mL, respectively. Naproxen decreases the in vitro LPS-induced PGE2 and TXB2 production in rats and humans with IC50 of 30.7 μM and 79.5 μM for PGE2 inhibition, 72.4 μM and 48.3 μM for TXB2 inhibition, respectively. Naproxen produces concentration-related inhibition of TXB2 production from human platelets and LPS-induced TXB2 production from human mononuclear cells with plC50 values (-log concentration inhibiting TXB2 by 50%) of 5.7 and 6.4, respectively, and exhibits slightly inhibitory selectivity for constitutive and induced COX-2 with IC50 COX-1/IC50 COX-2 of 6.3. Only high concentration of Naproxen can significantly induce apoptosis at 48 hours in HCA-7 colon cancer cells with IC50 of 1.45 mM.
in vivo Administration of Naproxen reduces the LPS-induced PGE2 and TXB2 production in vivo in rats with IC50 values of 12.8 μM and 5.9 μM, respectively, which represents that Naproxen is a nonselective COX inhibitor with the log IC50 ratio (COX-2/COX-1) of 0.34. Naproxen displays IC50 of 27 μM for analgesia in a rat model with carrageenan-induced arthritis and IC50 of 40 μM for antipyretics in a yeast-induced fever rat model, while exhibits inhibition of PGE2 with IC50 of 13 μM and TXB2 with IC50 of 5 μM.
特徴 Displays approximately equipotent inhibitory selectivity for COX-1 and COX-2 in intact cells.

プロトコル(参考用のみ)

キナーゼアッセイ COX-1 and COX-2 activities in intact cells
For the determination of COX-1 and COX-2 inhibition, bovine aortic endothelial cells (BAEC) are incubated for 30 minutes with Naproxen (0.1 ng/mL to 1 mg/mL), and cultured J774.2 macrophages are treated with endotoxin at 1 μg/mL for 12 hours to induce COX-2 followed by incubated for 30 minutes with Naproxen (0.1 ng/mL to 1 mg/mL), respectively. Arachidonic acid (30 μM) is then added, and the cells are incubated for a further 15 minutes at 37 °C. The medium is then removed, and radioimmunoassay is used to measure the formation of 6-keto-PGF1α, PGE2, thromboxane B2, or PGF2α for the assessment of IC50 for COX-1 and COX-2.
細胞アッセイ 細胞株 Human colon cancer HCA-7 cell lines
濃度 Dissolved in culture medium, final concentration ~20 mM
反応時間 24 and 48 hours
実験の流れ Cells are exposed to Naproxen for 24 and 48 hours, respectively. At the end of incubation, cells are harvested by trypsinization, stained with trypan blue solution (0.04% wt/vol) and counted in a Neubauer haemocytometer chamber for the determination of cell viability.
動物実験 動物モデル Male Sprague-Dawley rats
投薬量 2.5, 10 or 25 mg/kg
投与方法 Intravenously (i.v.) infusion or intraperitoneal (i.p.) injection

参考

  • https://pubmed.ncbi.nlm.nih.gov/8265610/
  • https://pubmed.ncbi.nlm.nih.gov/16682968/
  • https://pubmed.ncbi.nlm.nih.gov/7583521/
  • https://pubmed.ncbi.nlm.nih.gov/18033773/
  • https://pubmed.ncbi.nlm.nih.gov/21347567/

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Project IDentif.AI: Harnessing Artificial Intelligence to Rapidly Optimize Combination Therapy Development for Infectious Disease Intervention [ Adv Ther (Weinh), 2020, 2000034] PubMed: 32838027
Strain-Dependent Variability of Early Discovery Small Molecule Pharmacokinetics in Mice: Does Strain Matter? [ Drug Metab Dispos, 2020, 48(8):613-621] PubMed: 32474442

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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